Wesam Ali

Background: Seeds of Nigella sativa, commonly referred to as “black cumin”, are rich in a spectrum of biologically active substances and thus associated with a range of potential health benefits. Unlocking the activity of these phytochemicals traditionally requires solvent extraction. Previously, we have explored nanosizing as an alternative to liberate the biological activity of natural products, such as Solanum incanum, Pterocarpus erinaceus, Loranthus micranthus and Cynomorium coccineum. Objectives: Nanosizing natural products may increase their activity for a number of reasons ranging from an improved bioavailability to physical nano-toxicity. Because Nigella sativa is amenable to being “milled down”, this spice has been employed to explore the underlying causes of increased activity upon mechanical particle size reduction. Methods: Nigella sativa seeds were pre-milled employing a household flour mill followed by extensive grinding exploiting a planetary ball mill. The particles were characterized employing Laser Diffraction, Photon Correlation Spectroscopy and Scanning Electron Microscopy connected with Energy Dispersive X-ray Diffraction. Finally, the samples were evaluated for sterility profile, and nematicidal and antioxidant activities. Results: Suspensions containing fairly uniform particles of Nigella sativa showing diameters in the range of 100-1000 nm have been obtained. These nanosuspensions are characterized by considerably reduced microbial contamination when compared to the bulk material and reasonable antioxidant and nematicidal activities when employed at higher concentrations. This activity is comparable to the one of the ethanolic extract of the seeds and is significantly higher when compared to the one of aqueous extracts. A combination of “sterilization and extraction by milling”, improved liberation of soluble substances from small particles, surface activity and physical nano-activity of the particles itself is likely responsible for the activities observed. Conclusion: Nanosizing of the entire natural products provides an interesting alternative to solvent extraction as it results in the liberation of active ingredients and certain additional activities. The resulting nanosuspensions can be investigated further and optimized for applications in Nutrition, Agriculture, Medicine, and Cosmetics.

This study focuses on the design, synthesis, biological evaluation, and computer-aided structure-activity relationship (SAR) analysis for a novel group of aromatic triazine-methylpiperazines, with an hydantoin spacer between 1,3,5-traizine and the aromatic fragment. New compounds were synthesized and their affinities for serotonin 5-HT₆, 5-HT_1A, 5-HT_2A, 5-HT₇, and dopamine D₂ receptors were evaluated. The induced-fit docking (IFD) procedure was performed to explore the 5-HT₆ receptor conformation space employing two lead structures. It resulted in a consistent binding mode with the activity data. For the most active compounds found in each modification line, anti-obesity and anti-depressive-like activity in vivo, as well as “druglikeness” in vitro, were examined. Two 2-naphthyl compounds (18 and 26) were identified as the most active 5-HT₆R agents within each lead modification line, respectively. The 5-(2-naphthyl)hydantoin derivative 26, the most active one in the series (5-HT₆R: K_i = 87 nM), displayed also significant selectivity towards competitive G-protein coupled receptors (6–197-fold). Docking studies indicated that the hydantoin ring is stabilized by hydrogen bonding, but due to its different orientation, the hydrogen bonds form with S5.44 and N6.55 or Q6.58 for 18 and 26, respectively. Compound 26 exerted anxiolytic-like and antidepressant-like activities. Importantly, it demonstrated anti-obesity properties in animals fed palatable feed, and did not show toxic effects in vitro.

Selenium and selenocompounds have attracted the attention and the efforts of scientists worldwide due to their promising potential applications in cancer prevention and/or treatment. Different organic selenocompounds, with diverse functional groups that contain selenium, have been reported to exhibit anticancer and/or chemopreventive activity. Among them, selenocyanates, selenoureas, selenoesters, selenium-containing heterocycles, selenium nanoparticles, selenides and diselenides have been considered in the search for efficiency in prevention and treatment of cancer and other related diseases. In this review, we focus our attention on the potential applications of selenides and diselenides in cancer prevention and treatment that have been reported so far. The around 80 selenides and diselenides selected herein as representative compounds include promising antioxidant, prooxidant, redox-modulating, chemopreventive, anticancer, cytotoxic and radioprotective compounds, among other activities. The aim of this work is to highlight the possibilities that these novel organic selenocompounds can offer in an effort to contribute to inspire medicinal chemists in their search of new promising derivatives.

The goal of this study was to compare a Dye Binding Method with the standard Kjeldahl method in the context of protein determination in Ultra-Heat Treated (UHT) milk. Protein contents were determined in (25) samples of milk collected immediately post- ultra-heath treatment of milk and (25) samples collected after six-month storage at room temperature in Kjeldahl and Amido black methods. Samples digested using concentrated sulfuric acid at high temperatures and assayed using Automated Kjeldahl (Foss, Kjeltec™ 8200). Whereas, undigested samples were mixed with Amido Black a and density of color was measured against Amido black dilution series at wavelength of 620 nm. First stage: the average concentration of protein was (2.9256±0.01193 g/100 mL) versus (2.9396±0.01338 g/100 mL) using Kjeldahl versus Amido Black A respectively, with an average difference of (0,014). The concentrations ranged between (2.890-2.940 g/100 mL) and (2.910-2.960 g/100 mL) with a Coefficient of variation is (0.41%) and (0.46%) for Kjeldahl and Amido Black, respectively. (P) Value >0.0001. Therefore, there are no variances significantly different between two methods. Second stage: First stage: the average concentration of protein was (2.9224±0.03961 g/100 mL) versus (2.932±0.007071 g/100 mL) using Kjeldahl versus Amido Black A, respectively, with an average difference of (0.0096). The concentrations ranged between (2.770- 3.000 g/100 mL) and (2.920- 2.940 g/100 mL) with a Coefficient of variation is (1.36%) and (0.24) for Kjeldahl and Amido Black respectively. (P) Value

The investigation of natural products used in Traditional Medicine in Africa is complicated as modern analytical and screening methods are often not available. Computer aided product identification from traditional usage records (CAPITURE) may provide an interesting alternative and has been evaluated in the context of an ethnobotanical survey on fungal diseases and their traditional treatment in Tchamba District (Togo). 53 traditional healers were interviewed and their knowledge recorded. Several indicators, the Use Value (UV), Plant Part Value (PPV), Specific Use (SU) Value, Intraspecific Use Value (IUV) and Informant Consensus Factor (ICF), were applied to the data. Those indices, in addition to a bibliographic review, were then fed into a computer-aided approach which predicted two interesting plants out of the 43 species survey-recorded and their specific activities: Pterocarpus erinaceus sap against ringworm, Daniellia oliveri sap against intertrigo and respectively their roots and trunk barks against candidiasis. Subsequent laboratory-based studies have confirmed the predicted antimicrobial activities with MIC (128 μg/mL to 30 mg/mL) and without any notable toxicity on a normal human cell (MRC-5 cells). Although such a method may not be flawless, it is able to provide first leads, and in the face of limited resources, is an attractive alternative worth considering.