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Abstract Titanium dioxide nanoparticles (TiO2 NPs) have novel application and are used in many household application, nanomedicine, agriculture, industries and pharmaceutical products. These applications may be accompanied with potential risk in human health and the ecosystems. The current study was carried out to find out the acute damage that might be induced by TiO2 NPs in the heart and testis. Three groups of Wistar albino rats (Rattus norvegicus) were subjected to a single dose TiO2 NPs (126, 252, 378 mg/kg bw). Cardiac and testicular biopsies from each animal under study were handled for histological and histochemical examination. Rats exposed to TiO2 NPs demonstrated the following cardiac alterations: myofibres wavy appearance, myofibre disarray, partial cross striation, cardiomyocytes hydropic degeneration together with vacuolation and nuclear alterations. Moreover, acute exposure to TiO2 NPs induced the following testicular alterations: spermatocytes degeneration, spermatids sloughing and interstitial edema. The presented cardiac and testicular alterations were dose dependent. From the findings of the present study, it might be concluded that TiO2 nanomaterials are capable of inducing acute cardiac and testicular damage that is dose dependent and could adversely affect the function of the vital organs.

The antibacterial, anticancer, and wound-healing effects of honey can vary according to the type, geographical region, honey bee species, and source of the flowers. Nanotechnology is an innovative and emerging field of science with an enormous potential role in medical, cosmetics, and industrial usages globally. Metal nanoparticles that derived from silver and range between 1 nm and 100 nm in size are called silver nanoparticles (AgNPs). Much advanced research AgNPs has been conducted due to their potential antibacterial and anticancer activity, chemical stability, and ease of synthesis. The purpose of the present study was to explore the physicochemical properties of honey and the potential to use forest honey to synthesize AgNPs as well as to appraise the nanoparticles’ antimicrobial and anticancer effects. Here, we used three different percentages of forest honey (20%, 40%, and 80%) as biogenic mediators to synthesize AgNPs at room temperature. The development of AgNPs was confirmed by color change (to the naked eye) and ultraviolet-visible spectroscopy studies, respectively. The absorbance peak obtained between 464 to 4720 nm validated both the surface plasmon resonance (SPR) band and the formation of AgNPs. Regarding the sugar profile, the contents of maltose and glucose were lower than the content of fructose. In addition, the results showed that the SPR band of AgNPs increased as the percentage of forest honey increased due to the elevation of the concentration of the bio-reducing agent. A bacterial growth kinetic assay indicated the strong antibacterial efficacy of honey with silver nanoparticles against each tested bacterial strain. Honey with nanotherapy was the most effective against hepatocellular carcinoma (HepG2) and colon cancer (HCT 116) cells, with IC50s of 23.9 and 27.4 µg/mL, respectively, while being less effective against breast adenocarcinoma cells (MCF-7), with an IC50 of 32.5 µg/mL.

Background: The increasing rate of breast cancer globally requires extraordinary efforts to discover new effective sources of chemotherapy with fewer side effects. Glutaminase-free l-asparaginase is a vital chemotherapeutic agent for various tumor malignancies. Microorganisms from extreme sources, such as marine bacteria, might have high l-asparaginase productivity and efficiency with exceptional antitumor action toward breast cancer cell lines. Results: l-Asparaginase-producing bacteria, Bacillus velezensis isolated from marine sediments, were identified by 16S rRNA sequencing. l-Asparaginase production by immobilized cells was 61.04% higher than that by free cells fermentation. The significant productivity of enzyme occurred at 72 h, pH 6.5, 37°C, 100 rpm. Optimum carbon and nitrogen sources for enzyme production were glucose and NH4Cl, respectively. l-Asparaginase was free from glutaminase activity, which was crucial medically in terms of their severe side effects. The molecular weight of the purified enzyme is 39.7 KDa by SDS-PAGE analysis and was ideally active at pH 7.5 and 37°C. Notwithstanding, the highest stability of the enzyme was found at pH 8.5 and 70°C for 1 h. The enzyme kinetic parameters displayed Vmax at 41.49 μmol/mL/min and a Km of 3.6 × 10−5 M, which serve as a proof of the affinity to its substrate. The anticancer activity of the enzyme against breast adenocarcinoma cell lines demonstrated significant activity toward MDA-MB-231 cells when compared with MCF-7 cells with IC50 values of 12.6 ± 1.2 μg/mL and 17.3 ± 2.8 μg/mL, respectively. Conclusion: This study provides the first potential of glutaminase-free l-asparaginase production from the marine bacterium Bacillus velezensis as a prospect anticancer pharmaceutical agent for two different breast cancer cell lines.How to cite: Mostafa Y, Alrumman S, Alamri S, et al. Enhanced production of glutaminase-free L-asparaginase by marine Bacillus velezensis and cytotoxic activity against breast cancer cell lines. Electron J Biotechnol 2019;42. https://doi.org/10.1016/j.ejbt.2019.10.001. Keywords: Asparaginase, Bacillus velezensis, Breast cancer, Chemotherapy, Fermentation, Glutaminase, Immobilization, Marine, MCF-7 cells, Nitrogen, Production, Purification

In the present work, five naproxen derivatives, i.e., 3-amino-(4E)-5-imino-1-[2-(6-methoxy-2-naphthyl)propanoyl]-4-(benzylidene)-4,5-dihydro-1H-pyrazole (a), 3-amino-(4E)-5-imino-1-[2-(6-methoxy-2-naphthyl)propanoyl]-4-(4-bromobenzylidene)-4,5-dihydro-1H-pyrazole (b), 3-amino-(4E)-5-imino-1-[2-(6-methoxy-2-naphthyl)-propanoyl]-4-(4-methoxybenzylidene)-4,5-dihydro-1H-pyrazole (c), 3-amino-(4E)-5-imino-1-[2-(6-methoxy-2-naphthyl)propanoyl]-4-(4-methylbenzylidene)-4,5-dihydro-1H-pyrazole (d), 3-amino-(4E)-5-imino-1-[2-(6-methoxy-2-naphthyl)propanoyl]-4-(4-nitrobenzylidene)-4,5-dihydro-1H-pyrazole (e) were synthesized then characterized by FTIR, 1H and 13C NMR techniques. The ground state geometries were optimized by B3LYP functional of density functional theory (DFT) with three different basis sets (6-31G∗, 6-31G∗∗ and 6-31+G∗∗). The absorption wavelengths, oscillator strengths and major transitions were calculated using time dependent DFT. The effect of electron withdrawing groups (–NO2 and –Br) and electron donating groups (–CH3 and –OCH3) was intensively studied with respect to structure–activity relationship (SAR), quantitative structure–activity relationship (QSAR), frontier molecular orbitals (FMOs), molecular electrostatic potentials (MEP) and global reactivity descriptors. By the analysis of molecular docking work, it was found that pure hydrophobic substitution at position 4 of aldehyde part is more favorable than hydrophilic one. Compound c showed strong anti-proliferative activity against MCF-7 cells with IC50 value of 1.49 μM, and compound d showed moderate activity. The docking studies revealed that normal alkane chain is improving the biological activity in compound c, which endorsed to bury well in the active site resulting to enhance the hydrophobic interactions. The newly synthesized compounds against tested cell lines showed stronger antiproliferative activity as compared to the naproxen.

Kleinia pendula (Forssk.) DC. is a prostrate or pendent dark green succulent herb found in the southwestern mountain regions of Saudi Arabia. The literature survey of the plant reveals a lack of phytochemical and pharmacological studies, although traditional uses have been noted. The objective of the present work was to assess the in vivo analgesic and anti-inflammatory activities, as well as, the in vitro cytotoxic potential of the fractions of Kleinia pendula, and correlate these activities to the plant metabolites. The methanolic extract of Kleinia pendula was subjected to fractionation with n-hexane, ethyl acetate, chloroform, n-butanol, and water. The fractions were screened for their analgesic and anti-inflammatory activities, as well as cytotoxic activity against breast, liver, and colon cancer cell lines. The n-hexane and chloroform fractions of Kleinia pendula showed significant cytotoxic activity against all three cancer cell lines tested. The ethyl acetate and chloroform fractions showed significant analgesic and anti-inflammatory activities. The metabolites in these three active fractions were determined using UPLC-PDA-ESI-MS. Thus, the analgesic and anti-inflammatory activities of the plant were attributed to its phenolic acids (caffeoylquinic acid derivatives, protocatechuic, and chlorogenic acids). While fatty acids and triterpenoids such as (tormentic acid) in the hexane fraction are responsible for the cytotoxic activity; thus, these fractions of Kleinia pendula may be a novel source for the development of new plant-based analgesic, anti-inflammatory, and anticancer drugs.