Imène Becheker, Akram Melakhessou Mohamed, Eddine Marref Salah, Ismahene Grib, Amarouayache Mounia, Berredjem Malika, Berredjem Hajira
Research Laboratory of Interactions, Biodiversity, Ecosystems and Biotechnology, Faculty of Sciences, University August 20, 1955, 21000, Skikda, Algeria.
Laboratory of Applied Biochemistry and Microbiology, Faculty of Sciences, Badji Mokhtar University, 23000, Annaba, Algeria.
Chem Biodivers. 2023 Sep;20(9):e202300505. doi: 10.1002/cbdv.202300505. Epub 2023 Aug 10.
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 LC 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.
在过去几年中,由于其广泛的生物活性,对磺胺类药物的兴趣有所增加。它们灵活的结构使它们成为替代旧药物或开发现代多靶点药物的惊人候选者。在本研究中,对一系列新的磺胺类药物(sul1-5)进行了体外抗菌、细胞毒性和遗传毒性作用评估。针对12株临床菌株和4株参考菌株研究了抗菌活性。通过卤虫生物测定法进行细胞毒性活性测定,并在艾姆斯试验中评估遗传毒性。结果显示出有趣的抗菌活性,尤其是对革兰氏阴性菌。抑菌圈在15至30毫米之间,最低抑菌浓度(MIC)值在0.5至256微克/毫升之间。金黄色葡萄球菌分离株未显示抗菌活性。只有Sul1和Sul4对铜绿假单胞菌有活性。化合物Sul1和Sul2表现出显著的细胞毒性,LC分别等于18.29和18微克/毫升,并且对TA100和TA1535沙门氏菌菌株有遗传毒性作用。只有具有有趣抗菌活性、无细胞毒性和无遗传毒性作用的化合物Sul3、Sul4和Sul5可作为新药用于对抗耐药病原体。