Volume 34, Issue 1 (April 2023)
Studies in Medical Sciences 2023, 34(1): 35-45 |
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Research code: 94-01-36-9810
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Khabnadideh S, Sabet R, Zomorodian K, Divar M, Soleymani Gharbi F, Hassani B. EVALUATION OF ANTIFUNGAL, ANTIBACTERIAL AND CYTOTOXIC EFFECTS OF SOME NEW DERIVATIVES OF SPIROOXYINDOLES. Studies in Medical Sciences 2023; 34 (1) :35-45
URL: http://umj.umsu.ac.ir/article-1-5924-en.html
URL: http://umj.umsu.ac.ir/article-1-5924-en.html
Soghra Khabnadideh 
, Razieh Sabet * , Kamiar Zomorodian , Masoumeh Divar , Farnoush Soleymani Gharbi , Bahareh Hassani
, Razieh Sabet * , Kamiar Zomorodian , Masoumeh Divar , Farnoush Soleymani Gharbi , Bahareh Hassani
Assistant professor, Department of Medicinal Chemistry, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran (Corresponding Author) , sabet_r@sums.ac.ir
Abstract: (822 Views)
Background & Aims: In order to investigate the effects of new drugs, we decided to investigate twelve new derivatives with the basic structure of spirooxindoles that were previously synthesized for antimicrobial, antifungal and anticancer properties.
Materials & Methods: In this experimental study, we evaluated 12 spirooxyindole derivatives. The inhibitory effect of the compounds has been studied using broth microdilution method based on CLSI protocols on 16 different species of bacteria and fungi. Then, 6 compounds have been selected and their cytotoxicity effects on 2 cell lines MCF-7 and A-549 compared to doxorubicin have been investigated by MTT method. Excel 2013 software was used to perform statistical calculations of the results obtained from each experiment, and GraphPad Curve Expert 1.4 software was used to draw graphs and determine IC50 with a significance level of 0.05.
Results: At the concentration range of 1-512 μg/ml, the synthesized derivatives were not able to inhibit the growth or death of the investigated fungi and bacteria. Only the compound I12 at a concentration of 1000 μg/ml was able inhibit the growth of MFC-7 cell line by 49.23%.
Conclusion: Due to the lack of effective effect of these compounds in inhibiting the growth of bacteria and fungi, for the optimal use of these compounds in the treatment of fungal and bacterial infections, it is necessary to make more changes on their structures. Cytotoxicity assay reveals that the presence of the bulky ester in the N position of the isatin ring as well as the CN attached to the pyridine ring has been beneficial in the effectiveness of these derivatives.
Materials & Methods: In this experimental study, we evaluated 12 spirooxyindole derivatives. The inhibitory effect of the compounds has been studied using broth microdilution method based on CLSI protocols on 16 different species of bacteria and fungi. Then, 6 compounds have been selected and their cytotoxicity effects on 2 cell lines MCF-7 and A-549 compared to doxorubicin have been investigated by MTT method. Excel 2013 software was used to perform statistical calculations of the results obtained from each experiment, and GraphPad Curve Expert 1.4 software was used to draw graphs and determine IC50 with a significance level of 0.05.
Results: At the concentration range of 1-512 μg/ml, the synthesized derivatives were not able to inhibit the growth or death of the investigated fungi and bacteria. Only the compound I12 at a concentration of 1000 μg/ml was able inhibit the growth of MFC-7 cell line by 49.23%.
Conclusion: Due to the lack of effective effect of these compounds in inhibiting the growth of bacteria and fungi, for the optimal use of these compounds in the treatment of fungal and bacterial infections, it is necessary to make more changes on their structures. Cytotoxicity assay reveals that the presence of the bulky ester in the N position of the isatin ring as well as the CN attached to the pyridine ring has been beneficial in the effectiveness of these derivatives.
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