Evaluation of 2-Thioxoimadazolidin-4-one Derivatives as Potent Anti-Cancer Agents through Apoptosis Induction and Antioxidant Activation: In Vitro and In Vivo Approaches

Background: Hepatocellular carcinoma (HCC) is one of the most widespread malignancies and is reported as the fourth most prevalent cause of cancer deaths worldwide. Therefore, we aimed to investigate the probable mechanistic cytotoxic effect of the promising 2-thioxoimidazolidin-4-one derivative on liver cancer cells using in vitro and in vivo approaches. The compounds were tested for the in vitro cytotoxic activity using MTT assay, and the promising compound was tested in colony forming unit assay, flow cytometric analysis, RT-PCR, Western blotting, in vivo using SEC-carcinoma and in silico to highlight the virtual mechanism of action. Both compounds 4 and 2 performed cytotoxic effects against HepG2 cells with IC₅₀ values of 0.017 and 0.18 μM, respectively, compared to Staurosporine and 5-Fu as reference drugs with IC₅₀ values of 5.07 and 5.18 µM, respectively. Compound 4 treatment revealed apoptosis induction by 19.35-fold (11.42% compared to 0.59% in control), arresting the cell cycle at G2/M phase. Moreover, studying gene expression that plays critical roles in cell cycle and apoptosis by RT-PCR demonstrated that compound 4 enhances the expression of the pro-apoptotic genes p53, PUMA, and Caspase 3, 8, and 9, and impedes the anti-apoptotic Bcl-2 gene in the HepG2 cells. It can also inhibit the PI3K/AKT pathway at both gene and protein levels, which was reinforced by the in silico predictions of the molecular docking simulations towards the PI3K/AKT proteins. Finally, in vivo study verified that compound 4 has a promising anti-cancer activity through activating antioxidant levels (CAT, SOD and GSH) and ameliorating hematological, biochemical, and histopathological findings.     

Dynamical Analysis of a New Chaotic Fractional Discrete-Time System and Its Control

This article proposes a new fractional-order discrete-time chaotic system, without equilibria, included two quadratic nonlinearities terms. The dynamics of this system were experimentally investigated via bifurcation diagrams and largest Lyapunov exponent. Besides, some chaotic tests such as the 0–1 test and approximate entropy (ApEn) were included to detect the performance of our numerical results. Furthermore, a valid control method of stabilization is introduced to regulate the proposed system in such a way as to force all its states to adaptively tend toward the equilibrium point at zero. All theoretical findings in this work have been verified numerically using MATLAB software package.     

Polarity and steric effect of the lateral substituent on the mesophase behaviour of some newly prepared liquid crystals

Eight homologous series of 2- (or 3-) substituted phenyl 4?-(4?-alkoxy phenylazo) benzoates (In_a–h) were prepared in which, within each homologous series, the length of the terminal alkoxy group varies between 6, 8, 10 and 12 carbons, while the other substituent, X, is a laterally attached polar group that alternatively changed from CH₃, H, F, Br and CN. Compounds prepared were characterised by infrared and ¹H-NMR spectroscopy, and their mesophase behaviour investigated by differential scanning calorimetry and identified by polarised light microscopy. The results were discussed in terms of polarity and steric effects. The stability of the mesophase was correlated once with the dipolar anisotropy of the whole molecule and another with the dipolar anisotropy of the substituent, X. A comparative study was made between the investigated compounds and their previously prepared linear 4-substituted isomers, namely 4-substituted phenyl 4?-(4?-alkoxy phenylazo) benzoates (In_i–k).     

Characterization and catalytic performance of basaltic dust as an efficient catalyst in the liquid‐phase esterification of acetic acid with n‐butanol

Three natural basaltic samples were collected and used as efficient catalysts for the liquid‐phase synthesis of n‐butyl acetate. The samples were characterized by X‐ray fluorescence analysis (XRF), X‐ray diffraction (XRD), thermogravimetry (TG), differential thermal analysis (DTA), Fourier transform infrared (FT‐IR), scanning electron microscopy (SEM), and N₂ sorption. The acidity of the samples was determined using isopropanol dehydration, and the strength of the acid sites was measured using chemisorption of basic probes. The catalytic activity of the samples towards the esterification of acetic acid with n‐butanol was extensively examined. The influence of different parameters, such as the reaction refluxing time, molar ratio, catalyst loading, reusability, and calcination temperature, on the esterification reaction was studied in detail. The results revealed that all samples had high catalytic activity with a selectivity of 100% to n‐butyl acetate formation. In addition, the sample obtained from the top hill of Volcano had the highest activity with a 80% yield of n‐butyl acetate. Moreover, the significant catalytic performances were well correlated with the acidity of the samples and to the reaction rate constants.     

Promoting Effect of Soluble Polysaccharides Extracted from Ulva spp. on Zea mays L. Growth

Seaweeds can play a vital role in plant growth promotion. Two concentrations (5 and 10 mg/mL) of soluble polysaccharides extracted from the green macroalgae Ulva fasciata and Ulva lactuca were tested on Zea mays L. The carbohydrate and protein contents, and antioxidant activities (phenols, ascorbic, peroxidase, and catalase) were measured, as well as the protein banding patterns. The soluble polysaccharides at 5 mg/mL had the greatest effect on the base of all of the parameters. The highest effects of soluble polysaccharides on the Zea mays were 38.453, 96.76, 4, 835, 1.658, 7.462, and 38615.19, mg/mL for carbohydrates, proteins, phenol, µg ascorbic/mL, mg peroxidase/g dry tissue, and units/g tissue of catalase, respectively. The total number of protein bands (as determined by SDS PAGE) was not changed, but the density of the bands was correlated to the treatments. The highest band density and promoting effect were correlated to 5 mg/mL soluble polysaccharide treatments extracted from Ulva fasciata in Zea mays, which can be used as a biofertilizer.     

Phytochemical and In Silico ADME/Tox Analysis of Eruca sativa Extract with Antioxidant,Antibacterial and Anticancer Potential against Caco-2 and HCT-116 Colorectal Carcinoma Cell Lines

Eruca sativa Mill. (E. sativa) leaves recently grabbed the attention of scientific communities around the world due to its potent bioactivity. Therefore, the present study investigates the metabolite profiling of the ethanolic crude extract of E. sativa leaves using high resolution-liquid chromatography-mass spectrometry (HR-LC/MS), including antibacterial, antioxidant and anticancer potential against human colorectal carcinoma cell lines. In addition, computer-aided analysis was performed for determining the pharmacokinetic properties and toxicity prediction of the identified compounds. Our results show that E. sativa contains several bioactive compounds, such as vitamins, fatty acids, alkaloids, flavonoids, terpenoids and phenols. Furthermore, the antibacterial assay of E. sativa extract showed inhibitory effects of the tested pathogenic bacterial strains. Moreover, the antioxidant activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide (H₂O₂) were found to be IC₅₀ = 66.16 μg/mL and 76.05 μg/mL, respectively. E. sativa also showed promising anticancer activity against both the colorectal cancer cells HCT-116 (IC₅₀ = 64.91 μg/mL) and Caco-2 (IC₅₀ = 83.98 μg/mL) in a dose/time dependent manner. The phytoconstituents identified showed promising pharmacokinetics properties, representing a valuable source for drug or nutraceutical development. These investigations will lead to the further exploration as well as development of E. sativa-based nutraceutical products.