CYTOTOXICITY OF IMIDACLOPRID AND MYCLOBUTANIL PESTICIDES ON THREE CANCER CELL LINES

Three cancer cell lines, i.e. HEpG-2 (human liver carcinoma), MCF-7 (human breast adeno-carcinoma), and PC3 (Prostatic Small Cell Carcinoma) were used to determine the cytotoxic effects of the neonicotinoid insecticide (imidacloprid) and conazole fungicide (myclobutanil). Cytotoxicity was measured by neutral red incorporation (NRI) assay. The lowest concentration of the tested pesticides (0.5 μg/ml) was toxic. With the increase of the concentration up to 80 μg/ml, the Department of plant protection, Faculty of Agric., Ain Shams University, shoubra  Elkheima, Cairo, Egypt Department of Genetics, Faculty of Agric., Ain Shams University, Cairo, Egypt damage degree of the cellular form and size was more serious. The midpoint cytotoxicity value, (NRI50) for imidacloprid and myclobutanil for HEpG-2, MCF-7, and PC3 cancer cell lines were 110.5, 67.7 and 67.6 μg/ml and 38.12, 41 and 27.5 μg/ml, respectively. In general, myclobutanil was very toxic in the three cancer cell lines compared with imidacloprid

Genotoxicity assessment of amino zinc nanoparticles in wheat (Triticum aestivum L.) as cytogenetical perspective

This is the final version. Available on open access from Elsevier via the DOI in this record. Nanoparticles have a positive impact in several subjects especially in agriculture, while their safety is still being debated. Numerous commercial nano pesticide, insecticides, and fertilizers products are found in the local markets without any intensely studies on the side effect of these products on plant, human as well as environmental effects. The present study aimed to evaluate the genotoxicity of commercial amino zinc nanoparticles (AZ NPs) on Triticum aestivum L. during seeds germination and root elongation using concentration ranges (50, 100, and 150 ppm) at different exposure times (8, 16 and 24 hrs). Long term exposure to AZ NPs, exhibited only slight variation in germination rates and the elongation of roots was affected by AZ NPs treatment ranged from 97.66 to 100%. Significant reduction in the mitotic index was 35.33% after 24 hrs and 150 ppm of AZ NPs, was also observed comparing with control which was 88.0%. Genotoxicity was evaluated at a cytological level in root meristems that revealed sever variations in mitotic activity, chromosomal aberrations, and micronuclei release. Results exhibited that nano amino zinc could enter effortlessly into the cells and inhibit the normal cellular function. The decrease in the emergence of chromosomal aberrations resulting from AZ NPs exposure in a dose-dependent manner was clearly indicated that AZ NPs has induced genotoxic effect on wheat root tips.King Saud University, Riyadh, Saudi Arabi

Medical prospects of cryptosporidiosis in vivo control using biofabricated nanoparticles loaded with Cinnamomum camphora extracts by Ulva fasciata

Background and Aim: Global efforts are continuing to develop preparations against cryptosporidiosis. This study aimed to investigate the efficacy of biosynthesized Ulva fasciata loading Cinnamomum camphora oil extract on new zinc oxide nanoparticles (ZnONPs shorten to ZnNPs) and silver nanoparticles (AgNPs) as alternative treatments for Cryptosporidium parvum experimental infection in rats. Materials and Methods: Oil extract was characterized by gas chromatography-mass spectrometry, loaded by U. fasciata on ionic-based ZnO and NPs, and then characterized by transmission electron microscopy, scanning electron microscopy, and X-ray diffraction. Biosafety and toxicity were investigated by skin tests. A total of 105 C. parvum oocysts/rat were used (n = 81, 2–3 W, 80–120 g, 9 male rats/group). Oocysts shedding was counted for 21 d. Doses of each preparation in addition to reference drug were administered daily for 7 d, starting on post-infection (PI) day (3). Nitazoxanide (100 mg) was used as the reference drug. After 3 weeks, the rats were sacrificed for postmortem examination and histopathological examination. Two blood samples/rat/group were collected on the 21st day. Ethylenediaminetetraacetic acid blood samples were also used for analysis of biochemistry, hematology, immunology, micronucleus prevalence, and chromosomal abnormalities. Results: C. camphora leaves yielded 28.5 ± 0.3 g/kg oil and 20 phycocompounds were identified. Spherical and rod-shaped particles were detected at 10.47–30.98 nm and 18.83–38.39 nm, respectively. ZnNPs showed the earliest anti-cryptosporidiosis effect during 7–17 d PI. Other hematological, biochemical, immunological, histological, and genotoxicity parameters were significantly fruitful; hence, normalized pathological changes induced by infestation were observed in the NPs treatments groups against the infestation-free and Nitazoxanide treated group. Conclusion: C. camphora, U. fasciata, ZnNPs, and AgNPs have refluxed the pathological effects of infection as well as positively improved host physiological condition by its anticryptosporidial immunostimulant regenerative effects with sufficient ecofriendly properties to be proposed as an alternative to traditional drugs, especially in individuals with medical reactions against chemical commercial drugs

Synthesis of Novel 3H-Quinazolin-4-ones Containing Pyrazolinone, Pyrazole and Pyrimidinone Moieties

The diazonium salt of 3-(4-aminophenyl)-2-methyl-3H-quinazolin-4-one (2a) and its 6-bromo derivative 2b reacted with some active methylene compounds, namely ethyl acetoacetate (3), ethyl cyanoacetate (4) and acetylacetone (5), to afford the corresponding hydrazono quinazolinone derivatives 6-8. Treatment of 6a,b with hydrazine hydrate or phenyl hydrazine in refluxing ethanol afforded the corresponding pyrazolin-5-one derivatives of 3H-quinazolin-4-one 9a-d. Cyclization of 7a,b with hydrazine hydrate yielded the corresponding products 10a,b. Reaction of 8a,b with phenyl hydrazine or with urea afforded the corresponding derivatives 11a,b and 12a,b, respectively. Compounds 6-12 were identified by C,H,N analysis, IR, 1H-NMR, 13C-NMR and mass spectroscopy

Synthesis of Some Hydrazones and Osazones Containing Bromoquinazolines As Biologically Active Compounds

Condensation of 6-bromo-4-hydrazinoquinazoline (1) and 6,8- dibromo-4-hydrazinoquinazoline (2) with equimolar amounts of monosaccharides (3) afforded the corresponding hydrazones 4-11 in good yields that on acetylation gave the corresponding acetyl derivatives 12-19. However, reaction of three molar equivalent amounts of 1 and 2 with 3 afforded the corresponding osazones 20-27 in fair yields that on acetylation gave the corresponding acetyl derivatives 28-35. Some of the synthesized compounds have been proved to be biologically active as anticancer reagents

Synthesis and reactions of some 3 aryl-2-thioxoquinazolin-4(3H)-ones

A series of 3-aryl-2-thioxoquinazolin-4(3H)-ones 1a-g are prepared in good yields from reactions are prepared in good yields from reactions of anthranilic acids, aromatic amines and carbon disulfide under basic conditions in one step. Reaction of aminophenyl derivatives 1a,b with D-glucose affords the corresponding N-glucosylamines 4a,b in very good yields. Diaztoziation of 1a,b followed by reactions with aromatic amines yield the corresponding azo dyes 6a-f in 40-56% yields. The fastness of 6 has been studied. Compounds 6a,b,f have been proved to be biologically active

A simple procedure for synthesis of 3H-quinazolin-4-one hydrazones under mild conditions

Condensation of 6-bromo- and 6,8-dibromo-2-hydrazino-3-phenyl-3H-quinazolin-4-ones with d-sugars in the presence of a catalytic quantity of glacial acetic acid gave the corresponding hydrazones in good yields. Acetylation of hydrazones with acetic anhydride in anhydrous pyridine gave the corresponding acetyl hydrazones in high yields. Also, other hydrazones were synthesized from condensation of 2-hydrazino-3H-quinazolin-4-ones with aromatic aldehydes in the presence of a catalytic quantity of piperidine