Publications internationales
Résumé: Abstract Objective: Breast cancer (BC) is a heterogeneous disease with various biological and clinical subtypes. HER2 status (human epidermal growth factor receptor 2) is a crucial biomarker, associated with aggressive tumor behavior and poor prognosis. Advanced algorithmic models can aid in predicting cancer growth and metastasis, serving as valuable clinical tools for classification and treatment. Effective treatment strategies in oncology rely on accurate decision-making and early identification of factors associated with positive outcomes. Breast cancer (BC) presents challenges in understanding its contributing factors and establishing precise diagnostic methods. Our research introduces a novel method utilizing machine learning (ML) techniques to explore the relationship between various clinical and molecular variables focusing on predicting the status of the human epidermal growth factor receptor 2 (HER2), a key aggressiveness biomarker in BC. This objective aligns with leveraging artificial intelligence (AI) to support decision-making and address diagnostic considerations during treatment. Methods: Four ML models, namely logistic regression, random forest, LightGBM, and CatBoost, were implemented and evaluated using Python. The dataset was compiled by extracting medical records of BC patients, covering the period from 2018 to 2020. The model’s predictive performance was evaluated using accuracy, precision, recall, and F1-score as performance metrics. Result: The models achieved varying accuracies between 86.36 and 95.45%. The logistic regression model achieved an accuracy of 90.90% while the random forest and LightGBM models achieved an accuracy of 86.36%. The CatBoost model outperformed others with a greater accuracy of 95.45%, indicating its superior predictive capabilities for HER2 status. The ML models demonstrated potential in predicting HER2 status, enabling early detection and facilitating personalized treatment strategies. Conclusion: Our findings emphasize the significance of AI and ML techniques in improving BC outcomes and guiding decision-making. Further research is required to explore the broader applications of ML in predicting comprehensive BC outcomes in diverse healthcare settings and among heterogeneous populations.
Résumé: In this study, phytochemical and biological properties of Atriplex halimus and Haloxylon scoparium leaves, collected in Algeria, were evaluated. The aqueous extract of the studied plants was subjected to phytochemical screening by biochemical analysis and HPLC. The diffusion assay was assessed to investigate the antimicrobial effect against clinical and reference strains. Moreover, we investigated DPPH and FRAP, as well as the haemolytic activity. The results showed abundance in the phytochemical and mineral components. Notably, A. halimus exhibited the highest DPPH and FRAP values with IC50 = 1.69 ± 0.67 and IC50 = 3.20 ± 0.04 mg/g, respectively. The antibacterial activity was better at the concentration of 25 mg/mL, compared to the standard antibiotics. The inhibition zones varied between 8 and 40 mm. The haemolytic activity did not depict any toxicity. The investigated plants exhibited interesting antioxidant and antibacterial properties and may serve as a valuable source for novel antimicrobial drugs.
Résumé: In the last few years, the interest in sulfonamides has expanded owing to their broad spectrum of biological activities. Their flexible structure turns them into amazing candidates to replace old drugs or develop modern multi‐target agents. In this study, a series of new sulfonamides (sul1‐5) was evaluated, in vitro, for the antibacterial, cytotoxic and genotoxic effects. The antibacterial activity was investigated against 12 clinical and 4 reference strains. Cytotoxic activity was carried out by the brine shrimp bioassay and the genotoxicity was assessed in the Ames test. An interesting antibacterial activity was showed especially against Gram negative strains. The inhibition zones varied between 15 and 30 mm, and the Minimum Inhibitory Concentrations (MIC’s) values between 0.5 and 256 μg/ml. No antibacterial activity was shown with S. aureus isolates. Only Sul1 and Sul4 were active against P. aeruginosa. Compounds Sul1 and Sul2 showed a significant cytotoxicity with LC50 equal to 18.29 and 18 μg/ml respectively, and a genotoxic effect against TA100 and TA1535 Salmonella strains. Only compounds Sul3, Sul4 and Sul5 with an interesting antibacterial activity, no cytotoxicity and no genotoxic effects, could be exploited against resistant pathogens as new drugs.
Résumé: Background: Surgical site infections (SSIs) are one of the most common health care–associated infections in low and middle-income countries. The aims of this cross-sectional descriptive study were to estimate the frequency of postcaesarean infection with associated clinical characteristics and the antibiotic resistance profile of bacterial isolates. Methods: Patients who underwent a cesarean section at the obstetrics and gynecology department of the hospital in Annaba, Algeria were included. Each woman was followed postoperatively for 30 days and sociodemographic data were collected. Culture-based microbiological methods were used to identify the causative bacteria and determine their antibiotic resistance phenotype and molecular characterization. Results: Among 1,810 patients, we recorded 36 (1.9%) SSIs. Most patients had undergone an emergency delivery (75%) and low educational level (72.2%). The most frequent maternal pathologies were Body Mass Index ≥ 30 (63.9%), scarred uteri (58.3%), anemia (55.6%), and an American Society of Anaesthesiologists score between II and III (33.3%). Of the 43 bacteria isolated, Enterobacteriaceae were the most frequent (62.8%), predominated by Escherichia coli strains (43.5%), a majority of which were extended-spectrum βlactamases carriers (62.9%). Although gram-positive cocci were less frequent (37.2%), a majority ofEnterococcus faecalis (56.2%) were observed and 2 strains of vancomycin-resistant Enterococcus faecium harboring the vanA gene were identified. Conclusions: Extensive surveillance of at-risk populations should be integrated to prevent the occurrence of SSIs.
Résumé: Abstract: Monitoring water supply requires, among other quality indicators, the identification of the cyanobacteria community and taking into account their potential impact in terms of water quality. In this work, cyanobacteria strains were isolated from the Cheffia Reservoir and identified based on morphological features, the 16S rRNA gene, phylogenetic analysis, and toxin production by polymerase chain reaction PCR screening of the genes involved in the biosynthesis of cyanotoxins (mcyA, mcyE, sxtA, sxtG, sxtI, cyrJ, and anaC). Thirteen strains representing six different genera: Aphanothece, Microcystis, Geitlerinema, Lyngbya, Microcoleus, and Pseudanabaena were obtained. The results demonstrated the importance of morphological features in determining the genus or the species when incongruence between the morphological and phylogenetic analysis occurs and only the utility of the 16S rRNA gene in determining higher taxonomic levels. The phylogenetic analysis confirmed the polyphyly of cyanobacteria for the Microcystis and Oscillatoriales genera. Unexpectedly, Aphanothece sp. CR 11 had the genetic potential to produce microcystins. Our study gives new insight into species with picoplanktonic (or small) cell size and potentially toxic genotypes in this ecosystem. Thus, conventional water treatment methods in this ecosystem have to be adapted, indicating the requirement for pre-treatment methods that can effectively eliminate picocyanobacteria while preserving cell integrity to prevent toxin release.
Résumé: Abstract: Prostate cancer (PCa) is a major public health problem worldwide. Recent studies have suggested that ghrelin and its receptor could be involved in the susceptibility to several cancers such as PCa, leading to their use as an important predictive way for the clinical progression and prognosis of cancer. However, conflicting results of single nucleotide polymorphisms (SNPs) with ghrelin (GHRL) and its receptor (GHSR) genes were demonstrated in different studies. Thus, the present case–control study was undertaken to investigate the association of GHRL and GHSR polymorphisms with the susceptibility to sporadic PCa. A cohort of 120 PCa patients and 95 healthy subjects were enrolled in this study. Genotyping of six SNPs was performed: three tag SNPs in GHRL (rs696217, rs4684677, rs3491141) and three tag SNPs in the GHSR (rs2922126, rs572169, rs2948694) using TaqMan. The allele and genotype distribution, as well as haplotypes frequencies and linked disequilibrium (LD), were established. Multifactor dimensionality reduction (MDR) analysis was used to study gene–gene interactions between the six SNPs. Our results showed no significant association of the target polymorphisms with PCa (p > 0.05). Nevertheless, SNPs are often just markers that help identify or delimit specific genomic regions that may harbour functional variants rather than the variants causing the disease. Furthermore, we found that one GHSR rs2922126, namely the TT genotype, was significantly more frequent in PCa patients than in controls (p = 0.040). These data suggest that this genotype could be a PCa susceptibility genotype. MDR analyses revealed that the rs2922126 and rs572169 combination was the best model, with 81.08% accuracy (p = 0.0001) for predicting susceptibility to PCa. The results also showed a precision of 98.1% (p < 0.0001) and a PR-AUC of 1.00. Our findings provide new insights into the influence of GHRL and GHSR polymorphisms and significant evidence for gene–gene interactions in PCa susceptibility, and they may guide clinical decision-making to prevent overtreatment and enhance patients’ quality of life.
Résumé: The screening of PCa is based on two tests, the total PSA test and the rectal examination. However, PSA is not specific for PCa stage confirmation, leading in false-positive result and involving PCa over-diagnosis and over-treatment. HSP27 and Menin have been found to be overexpressed in a wide range of human cancers. Recent studies showed how HSP27 interacts with and stabilizes Menin to lead PCa progression and treatment resistance. The purpose of our study was to evaluate the correlation of HSP27 and Menin molecular expression, and their prognosis value in PCa with respect to clinicopathological features. Elisa was employed to measure serum HSP27 and Menin concentrations in 73 PCa patients and 80 healthy individuals. Immunohistochemistry (IHC) was used to determine HSP27 and Menin tissue expression in 57 tumors and 4 Benign Prostatic Hyperplasia (BPH) tissues. Serum HSP27 expression correlated with its tissue expression in all PCa patients, whereas serum Menin expression correlated only with tissue expression in aggressive PCa patients. Moreover, the results showed a positive correlation between HSP27 and Menin either in serum (r = 0.269; p = 0.021) or in tissue (r = 0.561; p < 0.0001). In aggressive PCa, serum expression of HSP27 and Menin was positively correlated (r = 0.664; R = 0.441; p = 0.001). The correlation between HSP27 and Menin expression in tissue was found only in patients with aggressive PCa (r = 0.606; R = 0.367; p = 0.004). Statistical analysis showed that the expression of both biomarkers was positively correlated with the hormone resistance or sensitivity, tumor aggressiveness, metastasis, Gleason Score, death and did not significantly correlate with age and PSA. Survival was illustrated by Kaplan–Meier curves; increased HSP27 and Menin expression correlated with shorter survival of PCa patients (p = 0.001 and p < 0.0001, respectively). Accuracy in predicting aggressiveness was quantified by the Area Under the Curve (AUC) of Receiver Operating Characteristic (ROC). We demonstrated that the combination of HSP27/Menin was statistically greater than PSA; it achieved an AUC of 0.824 (95% CI, 0.730–0.918; p < 0.0001). However, HSP27/Menin/PSA combination decreased the diagnostic value with an AUC of 0.569 (95% CI, 0.428–0.710; p = 0.645). Our work suggests the potential role of HSP27/Menin as diagnostic and prognostic biomarkers.
Résumé: The cyanobacteria management in water bodies requires a deep knowledge of the community composition. Considering the reliable and thorough information provided by the polyphasic approach in cyanobacteria taxonomy, here we assess the cyanobacterial community structure of the Cheffia reservoir from Algeria. Cyanobacteria were identified on the basis of morphological traits and next-generation sequencing (NGS); toxins-related genes were localized in addition to the identification of toxins; temperature and nutrient level of water samples were also determined. The polyphasic approach was essential for cyanobacteria investigation; 28 genera were identified through 16S rRNA metabarcoding with the dominance of taxa from Microcystis (34.2%), Aphanizomenon (20.1%), and Planktothrix (20.0%), and morphological analysis revealed the association in this water body of five species within the genus Microcystis: M. aeruginosa, M. novacekii, M. panniformis, M. ichthyoblabe, and M. flos-aquae. The presence of mcyE genotypes was detected; moreover, HPLC–PDA and LC–ESI–MS/MS revealed the production of microcystin-LR. Results obtained in our study are very important since this ecosystem is used for water supply and irrigation; as a consequence, a good water management plan is essential.
Résumé: The Pharmaceutical companies are very interested in thediscovery of new natural bioactive molecules with an impoortant effect andless toxicity, in order to replace old drugs, especially antibiotics which hadlost their effectiveness following the spread of multi-resistant bacteria. Thisstudy was aimed to investigate, in vitro, some extracts (aqueous extracts,oily extracts and essential oils) of arabic and myrrh gums, plant exudatescommonly used in folk medicine for treating several diseases. The antimicrobial activity against clinical bacterial and fungalstrains was carried out using disk diffusion and broth dilution methods.Cytotoxic activity was mesured using the brine shrimp lethality bioassaydetermining the LC50 and genotoxic activity by the preincubation Ames Testusing Salmonella strains TA100, TA98 and TA1535 treated with or withoutthe metabolic activation (S9 fraction). An interesting antimicrobialactivity was demonstrated, especilly against Gram negative strains.Inhibition zones vary between 16 and 30 mm and MIC’s values between15.62 and 250 μg/ml. All the tested extracts exhibited a bactericidal activity.The arabic gum extracts showed no cytotoxic effect with LC50 > 100 μg/ml.Myrrh gum extracts showed a significant toxicity to the brine shrimp naupliiwith LC 50 < 100 μg/ml. Results of the Ames test indicated that all testedextracts did not possess genotoxic potential. Our studyhighlighted the antimicrobial potential of gums extracts, making them anexcellent drug candidates against resistant pathogens.
Résumé: Fructose consumption is associated with the development of obesity and metabolic syndrome (MetS) in human and animal models. Objective: This study investigates the ability of an aqueous extract of Artemisia herba-alba Asso (AH) to ameliorate fructose-induced MetS in Male Wistar rats. Methods: AH extract at doses of 100, 200 and 400 mg/kg b.w./day was administered for six weeks to MetS animals. Results: Liquid fructose (10% w/v) intake did not vary total animal body weight, whereas, it produced moderate hyperglycemia associated with metabolic and histological alterations. Treating MetS rats with AH extract improved insulin sensitivity, alleviated atherogenic dyslipidaemia and decreased lipid deposition in their hepatic tissues. Additionally, AH extract was found to raise GSH level and antioxidant enzymes (GPx, GST and CAT) activities in rat livers homogenates. Conclusion: The results here reported demonstrated, for the first time, that A. herba-alba have therapeutic proprieties against fructose-induced MetS in rodent model.
Résumé: A series of new azo disperse dyes was synthesized by coupling 4-hydroxy-6-methyl-2H-pyran-2-one (triacetic acid lactone, TAL) or its hydrogenated derivative 4-hydroxy-6-methyl-5,6-dihydro-2H-pyran-2-one (dihydro triacetic acid lactone, DHTAL) with diazonium salts derived from aniline, 4-bromoaniline, 4-nitroaniline, 4-methoxyaniline, 2,4-dimethoxyaniline and 2,5-dimethoxyaniline. Spectroscopic data of these dyes dissolved in five organic solvents were measured. The effects of solvent polarity, nucleophilic component and substituent nature on the visible absorption spectra of the dyes are also reported. The structures of all compounds were confirmed by FT-IR, electronic absorption in UV and visible regions, 1H, 13C and 2D NMR and high resolution mass spectroscopy (HRMS). In addition, in vitro antibacterial activity of the synthesized derivatives against Gram positive and Gram negative bacteria, both reference and clinical strains, was evaluated qualitatively and quantitatively by agar diffusion method.
Résumé: Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), α-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, β-amino esters, and oxazolidin-2-ones). All structures were confirmed by 1H, 13C, and 31P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their in vitro antibacterial activity against four reference bacteria including Gram-positive Staphylococcus aureus (ATCC 25923), and Gram-negative Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Pseudomonas aeruginosa (ATCC 27853), in addition to three clinical strains of each studied bacterial species. Compounds 1a–7a and 1b showed significant antibacterial activity compared to sulfamethoxazole/trimethoprim, the reference drug used in this study.
Résumé: Prostate cancer (PCa) is a major public health problem worldwide, with high morbidity and mortality levels. Advanced age, androgen stimulation, and ethnicity have been reported to be possible risk factors. It has been suggested that particular genetic polymorphisms in glutathione S-transferases (GST), xenobiotic-metabolising enzymes, could predispose to prostate cancer through heritable deficiency in detoxification of environmental carcinogens. Conflicts in the published results and the absence of similar in depth studies in Algeria prompted us to perform the present case-control study of GSTM1 and GSTT1 polymorphisms and their possible association with PCa in an Algerian population. Methods We determined GSTM1 and GSTT1 genotypes for 49 histologically verified prostate cancer patients and in 41 age-matched healthy controls by multiplex polymerase chain reaction (PCR) using peripheral blood DNA samples. Result While an association between the GSTM1 null genotype and PCa risk (OR= 3.69, 95% CI= 1.30-10.44; P = 0.01) was evident, the GSTT1 null genotype (OR= 0.92, 95% IC= 0.32-2.62; P = 0.49) appeared without influence. Furthermore, no statistically significant differences between the double null genotype and PCa is detected, also no statistically significant differences between smoking status and PCa is detected. Conclusion The GSTM1 null genotype may increase individual susceptibility to prostate cancer. On the other hand, the null-activity genotype of GSTT1 did not appear to contribute to the risk of prostate cancer in our population.
Résumé: Acute toxoplasmosis in pregnant women presents a high risk of Toxoplasma transmission to the fetus. Early diagnosis is difficult, especially when serological testing for IgG/IgM antibodies fail to differentiate between a recent and a past infection. In this case, we rely on IgG avidity or PCR assays. Objectives The aim of this study was to compare conventional ELISA and IgG avidity, with PCR using B1 and P30 primers for the early diagnosis of toxoplasmosis in pregnant women. Methods Sera were collected from 143 pregnant women and measured by ELISA for anti-Toxoplasma IgG, IgM, IgA and IgG avidity. DNA was extracted from 57 peripheral blood and 14 amniotic fluid samples for PCR amplification. Results A total of 57 out 143 women were seropositive: 30 (52.6%) were IgG+/IgM− and 27 (43.8%) were IgG+/IgM+; IgA antibodies were positive in 7 (12.2%) cases. IgG avidity was low in 9 women suggesting an acute infection; 3 women presented an intermediate avidity. PCR detected Toxoplasma DNA in 9 women presenting low avidity and was negative for the intermediate avidity cases. Conclusion PCR combined to avidity IgG performed better than ELISA IgG, IgM and/or IgA assays alone. PCR was useful in the case of intermediate avidity.
Résumé: Acute toxoplasmosis in pregnant women presents a high risk of Toxoplasma transmission to the fetus. Early diagnosis is difficult, especially when serological testing for IgG/IgM antibodies fail to differentiate between a recent and a past infection. In this case, we rely on IgG avidity or PCR assays. Objectives The aim of this study was to compare conventional ELISA and IgG avidity, with PCR using B1 and P30 primers for the early diagnosis of toxoplasmosis in pregnant women. Methods Sera were collected from 143 pregnant women and measured by ELISA for anti-Toxoplasma IgG, IgM, IgA and IgG avidity. DNA was extracted from 57 peripheral blood and 14 amniotic fluid samples for PCR amplification. Results A total of 57 out 143 women were seropositive: 30 (52.6%) were IgG+/IgM− and 27 (43.8%) were IgG+/IgM+; IgA antibodies were positive in 7 (12.2%) cases. IgG avidity was low in 9 women suggesting an acute infection; 3 women presented an intermediate avidity. PCR detected Toxoplasma DNA in 9 women presenting low avidity and was negative for the intermediate avidity cases. Conclusion PCR combined to avidity IgG performed better than ELISA IgG, IgM and/or IgA assays alone. PCR was useful in the case of intermediate avidity.
Résumé: In this study, we examined the antihyperglycemic and antidiabetic effects of a novel synthesized molecule, the Ethyl (S)-2-(1-cyclohexylsulfamide carbamoyloxy) propanoate (ESP1b), in streptozotocin (STZ)-induced diabetic Wistar rats. Experimental diabetes mellitus was produced by a single intraperitoneal injection of STZ (55 mg/kg b.w.). Seven day postinjection, animals have received ESP1b orally at the doses of 5, 10 and 20 mg/kg b.w. daily for 28 day. This resulted in a clear decline, in a dose dependent manner, of blood glucose levels during the oral glucose tolerance test (OGTT) and the four weeks of treatment period. ESP1b at 20 mg/kg b.w. has alleviated body weight loss, improved plasma insulin concentration and at the same time markedly decreased the values of glycosylated hemoglobin, lipoproteins and atherogenic ratios. Additionally, ESP1b notably restored renal as well as hepatic functions tests. Histopathological examinations of pancreatic tissue also confirmed the previous biochemical findings. Considering the obtained results, it may be concluded that ESP1b possess a potent antihyperglycemic activity in STZ-diabetic rats possibly related to an insulin-secretagogue effect, which may be responsible for the moderate decrease in blood glucose concentration observed in normal rats dministrated with this tested compound.
Résumé: A series of four substituted sulfonamide derivatives 1a-d were evaluated, in vitro, for the antibacterial and cytotoxic activities against 216 clinical Gram-negative bacteria, and three reference strains: E. coli ATCC 25922, K. pneumoniae ATCC 700603 and P. aeruginosa ATCC 27853. The antibacterial effect of synthesized compounds was investigated by using the disk diffusion method to evaluate the inhibition zones. The MIC values were determined by the dilution broth method; the MIC50 and MIC90 were calculated. The cytotoxic properties of the tested compounds were carried out, in vitro, by the brine shrimp bioassay. The results showed that the tested compounds have significant antibacterial activity against the clinical isolates, excepted S. odorifera and C. freundii. No antibacterial activity was shown whith the sulfonamide 1a against the clinical isolates. Only the sulfonamide 1a showed a significant cytotoxicity to the brine shrimp nauplii with LC50 equal to 18, 29 µg/ml. It may be concluded that promising innovative compounds 1b-d, with high antibacterial activity and no toxicity effect, could be exploited against resistant pathogens.
Résumé: The Heavy metal cadmium (Cd) pollution is a major concern worldwide. It is a dangerous environmental toxicant that can be lethal to humans and other organisms. The current study was designed to investigate the toxicity of Cd on the oxidative stress biomarkers and the respiratory metabolism of an alternative unicellular model, Paramecium sp. Four Cd concentrations were used: 0.5; 1; 2 and 5 mM. Stress generated by the metal was assessed on cellular growth, respiratory metabolism, antioxidant enzymatic activity (GSH, GST and Cat) and reactive oxygen species variations (ROS). The outcomes of this investigation revealed that Cd is lethal to the protozoan Paramecium sp. since the first lowest concentration, showing a concentration dependent decrease of the cell number. Our results highlight an inhibitory effect of Paramecium sp. respiratory metabolism. A time dependent increase in antioxidant enzymes, including catalase (CAT) and glutathione-s-transferase (GST) associated with ROS production, and a time dependent decrease in reduced glutathione (GSH) was observed. In summary, our study shows, that the Cd is involved in the induction of an oxidizing stress expressed by, a cell growth disturbance, a respiratory metabolism disruption and a stimulation of ROS production. The results also highlight significant antioxidant capacity induced in Paramecium sp.
Résumé: The present study aimed to investigate the effects of the 3, 4-dihydroisoquinolin-2(1H)-sulfonamide on blood glucose, lipid profile, hepatic and renal functions and enzyme activities in alloxan-induced diabetic Wistar rats. Experimental diabetes was produced by a single intraperitoneal injection of alloxan (140 mg kg-1 b.wt.). Three groups of diabetic rats were administered orally with two doses of the novel sulfonamide (2.5 and 5 mg kg-1 b.wt.) and a standard drug, glibenclamide (2.5 mg kg-1 b.wt.), for 10 days. Changes in body weight, food consumption, water intake and blood glucose levels were recorded regularly. At the end of the treatment period, blood was collected to determine biochemical parameters and enzyme activities in serum samples. Pancreas, liver, kidneys, spleen and heart were weighed in order to evaluate the relative organ weight. Histological changes in pancreas were examined by microscopy according to procedure with hematoxylin-eosin. The treatment with 2.5 and 5 mg kg-1 of the tested compound decreased the pathophysiological disturbances of diabetic syndrome. A significant (p<0.001) anti-hyperglycemic activity was clearly observed from the 4th day. Significant decreases (p<0.05) in total lipid and total cholesterol levels and highly significant decreases (p<0.001) in the level of Triglyceride were also noted with the two doses of the tested compound. Moreover, renal and hepatic functions were improved and lesions of pancreas were reversed in treated animals. However, the tested compound at 5 mg kg-1 produced highly significant increase (p<0.001) in the relative spleen weight. Our findings suggest that the 3, 4-dihydroisoquinolin-2(1H)-sulfonamide is endowed with an interesting anti-diabetic activity comparable to glibenclamide; however, it could present an immunological risk, so further more studies must be undertaken.
Résumé: Two novel sulfonamide derivatives, the 3,4-dihydroisoquinoline-2(1H)-sulfonamide (1a) and the 4phenylpeperazine sulphonamide (1b), have been evaluated in vitro as antibacterial agents against urinary and standard strains of Gram-negative Escherichia coli, by both disk diffusion and dilution assay methods. These bacteria were screened against the novel compounds which were compared to a standard antibiotic, the sulfamethoxazol-trimethoprim (STX). The results revealed that the tested compounds showed a good antibacterial activity. The diameters of the growth inhibition area were in the range 10-40 mm. Antibacterial activity of compound 1a, against all the bacterial strains, was superior to those of the compound 1b and the commercial drug SXT. The diameters of the growth inhibition area of sulfonamide 1a were in the range 15-40 mm and the MICs were ranged from 2 to 128 g/ml. Compound 1b was less active than compound 1a but more active than antibiotic SXT. Diameters of inhibition of compound 1b were in the range 4-26 mm and the MICs were ranged from 8 to 256 µg/ml. In conclusion, the newly synthesized sulfonamide derivatives showed a powerful interesting antibacterial activity against all strains of Escherichia coli. Better activity was obtained with compound 1a.
Publications nationales
Résumé: Genotoxic property of four new antibacterial sulfonamides 1a-d has been evaluated in thisstudy using two standard genotoxicity assays: the Salmonella typhimurium mutagenicity assayor Ames test based on the use of Salmonella strains TA100, TA98 and TA1535, treated withand without metabolic activation (S9 mix fraction) and the SOS ChromtestT M Kit assay usingEscherichia coli PQ 37.From the results of the Ames test we note that only 1c (N-(phenyl) sulfamide) showed nogenotoxic effect, contrary to 1a [(N-(4-methoxyphenyl) sulfamide], 1b [(N-(3-fluorophenyl) sul-famide] and 1d [(N-(phenylethyl) sulfamide] that have showed genotoxic effect with and with-out metabolic activation. Results of the SOS Chromotest confirmed these. Sulfonamides 1a, 1band 1d expressed the genotoxic potential by stimulating the production of β-galactosidase. Thegenotoxic effect of these molecule is strictly linked to their carcinogenic potential. So, from ourresults, we suggested that only compound 1c was non-genotoxic and safe to be tested, eventually,in vivo. Furthermore, we conclude that genotoxic effect depends essentially on the structure andcomposition of the molecule. (PDF) Ames test and SOS Chromotest to Evaluate the Genotoxicity Effect of Synthesized Series of Antibacterial Sulfonamides. Available from: https://www.researchgate.net/publication/371951798_Ames_test_and_SOS_Chromotest_to_Evaluate_the_Genotoxicity_Effect_of_Synthesized_Series_of_Antibacterial_Sulfonamides [accessed Mar 23 2025].