Physicochemical and ecotoxicological approaches for Moknine Continental Sebkha in Tunisia.

Degradation of water quality is an emerging issue in many developing countries. In this context, industrial and domestic effluents heavily contaminate the coast of Moknine Continental Sebkha in Tunisia. The present study aimed to biomonitor the seawater quality of the Moknine Continental Sebkha coast using physicochemical and ecotoxicological approaches. The ecotoxicological assessment was performed using three species representing different trophic levels, namely Vibrio fischeri, Selenastrum capricornutum, and Lepidium sativum. In the physicochemical analysis such as BOD (biochemical oxygen demand), COD (chemical oxygen demand), TSS (total suspended solids), TOC (total organic carbon), NO3- (nitrate), AOX (adsorbable organic halogen), the recorded levels of pH and total suspended solids did not comply with the Tunisian standard (NT.09.11/1983). The ecotoxicological data confirmed that the tested water samples displayed toxicity to two test indicators L. sativum and S. capricornutum. A targeted chemical screening of the Moknine Continental Sebkha coast previously performed revealed the presence of total mercury, four phthalate acid esters, and one non-phthalate plasticizer, a fact that could explain the observed ecotoxicological effects and therefore might harm the biotic area and the health of the surrounding population.

Evaluating the effect of dermaseptin S4 and its derivatives on multidrug-resistant bacterial strains and on the colon cancer cell line SW620.

Dermaseptins are peptides found in the skin secretions of Phyllomedusinae frogs. These peptides exert a lytic action on various microorganisms and have no considerable hemolytic effect except dermaseptin S4 (DS4) which exhibits a powerful cytotoxic effect. Therefore, we synthesized several analogs of DS4 in an attempt to find molecules with a weak hemolytic effect and significant bioactivities. In this study, we performed the synthesis of truncated peptides by introducing C-terminal and N-terminal amino acid deletions of the native sequence. All peptide analogs, in comparison with parental peptide, were tested firstly on human red blood cells to work out their cytotoxicity, secondly on the multidrug-resistant bacteria by trying to find MICs, and finally on colon cancer tumor cell line SW620 using the MTT test so as to investigate the anti-proliferative effect. Our results showed that, on the one hand, the N terminus of the native peptide was necessary for the antibacterial activity and the anti-proliferative effect of the peptide. On the other hand, the hemolytic activity was more notable in the sequences broken down on the C-terminal side.

Partial characterization and antitumor activity of a polysaccharide isolated from watermelon rinds.

As a health-beneficial fruit, watermelon is widely consumed by people around the world. However, components responsible for the health benefits are not yet determined. As watermelon contains a large amount of polysaccharides, these carbohydrates might play an important role in the health benefits. In this work, polysaccharide from watermelon rinds (PWR) was extracted by papain digestion, purified and characterized by GC-MS, SEC/MALS/VD/DRI, FTIR and 1D and 2D NMR which revealed the glycosidic linkages, their locations in branches and backbone. The monosaccharide composition revealed that the extracted polysaccharide was composed of galactose (38.26%), arabinose (26.12%), rhamnose (17.86%), mannose (9.94%), xylose (5.10%) and glucose (2.70%) with a percentage of uronic acid of 45%. A combination of CPG and NMR analysis showed that the extracted polysaccharide is arabinogalactan linked to type I rhamnogalacturonan. we notice that the arabinogalactan was formed by →6)-ß-D-Galp-(1→ as backbone with short branching of arabinose linked in α 1 → 3, rhamnose linked in α 1 → 4, mannose linked in ß 1 → 6 and galactose branches linked in ß 1 → 3. Furthermore, PWR exhibited obvious cytotoxicity ability to human laryngeal carcinoma Hep-2 cells in a dose-and time-dependant manner.

Human urine contamination with environmental pollutants: simultaneous determination using UPLC-MS/MS.

Paraben derivatives are widely used as an antifungal, antimicrobial preservative in cosmetic products, pharmaceuticals, and food. These molecules are called endocrine disruptors (EDCs). The exposure of the human body to paraben derivatives needs further study and for this purpose 200 urine samples were collected from Tunisian men and women aged between 5 and 90 years to determine three paraben derivatives: methylparaben (MP), ethylparaben (EP) and propylparaben (PP) using ultra performance liquid chromatography-tandem mass spectrometer (UPLC-MS/MS). The three major parabens were found in 95 urine samples. The obtained results indicate that MP, EP, and PP were detected in 57%, 46%, and 40% of all samples, respectively. Urinary concentration for the three parabens was in the range of 0.88-84.46 ng/mL, 0.52-29.2 ng/mL, and 0.51-28.17 ng/mL of PP, MP, and EP, respectively. In addition, the concentrations of the paraben derivatives in women were higher than those of men. These findings indicate that the exposure occurs from common products (foods, cosmetics, and pharmaceuticals). The Tunisian authorities should control the composition of packaging of these common products in order to protect humans against EDCs.

Dermaseptins as potential antirabies compounds.

Over the last 20 years, natural peptides playing a key role in defense mechanisms and innate immunity have been isolated from unicellular organisms. Amphibian skin secretes dermaseptins, 24-34 amino acids in length that have a wide antimicrobial spectrum incorporating yeast, fungi, protozoa, bacteria and enveloped viruses. The anti-rabies virus (RABV) activity of dermaseptins S3 (30aa) and S4 (28aa) from Phyllomedusa sauvagei has been investigated, and further dissected its molecular basis by comparing punctual mutation or deletion of S4 analogues. The results showed that: (1) S4 is more active than S3 against RABV infection, 89% versus 38% inhibition at 7.5 µM; (2) the 5 NH2-aa of S4 are crucial for its inhibitory potential (S46-28 lost any inhibition) but the COOH terminus stabilizes the inhibitory potential (S41-16 showed only 23% inhibition at 7.5 µM); (3) there is a correlation between viral inhibition and dermaseptin cytotoxicity, which remains however moderated for BSR cells (≤12% at 10 µM). A single mutation in position 4 (S4M4K) slightly reduced cytotoxicity while keeping its antiviral activity, 97% at 7.5 µM. S4 and S4M4K showed an antiviral activity in vitro when provided 1 h after infection. In vivo experiments in mice by intramuscular injection of non-toxic doses of dermaseptin S4M4K 1 h post-infection by a lethal dose of RABV at the same site allowed more than 50% improvement in mice survival. This study highlights the potential interest of dermaseptins as non-expansive alternatives to rabies immunoglobulins for the treatment of rabies that continues to claim about 60,000 human lives per year worldwide, almost exclusively in developing countries.

Preliminary evaluation of plasticizer and BPA in Tunisian cosmetics and investigation of hazards on human skin cells.

In this study, 18 plasticizer (phthalates, adipates, sebacates, and others) and BPA residues in some cosmetic samples collected from Tunisian market are evaluated by micro-matrix solid-phase dispersion combined with GC-MS. In parallel, the impact of these molecules and the cosmetics in the human epithelial cell lines is investigated. The cytotoxic activity of cosmetic extracts is evaluated in vitro against B16 and Hep-2 human skin cell lines using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide assay. This study shows that the tested cosmetic products could constitute a hazard to the consumer health and wellness and that strict safety analysis on cosmetic products needs to be carried out before they are marketed.

Spermicidal activity of dermaseptins.

OBJECTIVE: The present study was undertaken to elucidate the spermicidal efficacy of two synthetic antimicrobial peptides, dermaseptin (DS1 and DS4). METHODS: Twenty samples of fresh semen were obtained from patients aged between 23 and 35 years. The ability of DS to kill sperm was evaluated by the Sander-Cramer test under in vitro conditions. RESULTS: The data showed that sperm motility was inhibited with various concentrations of DS at different intervals ranging from 2 to 240 min. The effective 100% inhibitory concentration (EC(100)) of DS4 in 2 min during the sperm immobilization assay was 100 microg/mL whereas the sperm immobilization of EC(100) of DS1 was 200 microg/mL. The presence of 0.1% chelating agent ethylenediaminetetraacetic acid (EDTA) reduced the EC(100) of DS4 to 10 microg/mL whereas less than a two-time enhancement in DS1 activity was observed upon combination with EDTA. The action of DSs on sperm motility was observed to be dose dependent. Supplementation with pentoxifylline and that with calcium are known to enhance the motility of sperm but they did not prevent the spermicidal action of DSs. CONCLUSION: This present study indicates that DS is an effective agent to kill sperm. In view of this fact, it is suggested that DS4 has antibacterial, antiviral, antifungal and potentially spermicidal activities and could be a potent vaginal contraceptive.

The antimicrobial peptide dermaseptin S4 inhibits HIV-1 infectivity in vitro.

Most of HIV-1 infections are acquired through sexual contact. In the absence of a preventive vaccine, the development of topical microbicides that can block infection at the mucosal tissues is needed. Dermaseptin S4 (DS4) is an antimicrobial peptide derived from amphibian skin, which displays a broad spectrum of activity against bacteria, yeast, filamentous fungi, and herpes simplex virus type 1. We show here that DS4 inhibits cell-free and cell-associated HIV-1 infection of P4-CCR5 indicator cells and human primary T lymphocytes. The peptide is effective against R5 and X4 primary isolates and laboratory-adapted strains of HIV-1. Its activity is directed against HIV-1 particles by disrupting the virion integrity. Increasing the number of DS4-positive charges reduced cytotoxicity without affecting the antiviral activity. The modified DS4 inhibited HIV-1 capture by dendritic cells and subsequent transmission to CD4(+) T cells, as well as HIV-1 binding on HEC-1 endometrial cells and transcytosis through a tight epithelial monolayer.