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Bioactivity and DNA/BSA Interactions of Selenium N‐Heterocyclic Carbene Adducts
ChemistrySelect ( IF 1.9 ) Pub Date : 2020-09-16 , DOI: 10.1002/slct.202001990
Rizwan Ashraf 1 , Muhammad Adnan Iqbal 1, 2 , Haq Nawaz Bhatti 1 , Muhammad Ramzan Saeed Ashraf Janjua 3 , Mohamed El‐Naggar 4
Affiliation  

In wake of promising biomedical applications of organo‐selenium compounds, the present work was planned to synthesize selenium adducts (1 s‐4 s) and their respective azolium ligands (1 a4 a), which were subsequently authenticated by various analytical and spectroscopic techniques like microanalysis, UV‐Visible, FT‐IR, 1H & 13C NMR and Electrospray Ionisation‐Mass Spectrometry (ESI‐MS). Moreover, the synthesized compounds were tested for their biological potential like antioxidant, antimicrobial, hemolytic, DNA and Bovin Serum Albumin (BSA) interactions, stability and lipophilicity using in‐vitro models. All the compounds were found stable in solution form for studied period 12–68 hours and showed good lipophilic values in the range of logP 0.66–0.85. In context to biological activities, selenium compounds showed better antimicrobial (ranging 17.4±0.5–25.3±0.8 mm against S. aureus and 18.6±0.7–24.1±0.9 against E.coli at concentration of 0.3 mg/mL for both strains) and antioxidant potential (IC50 ranging 40.0–62.0 μg/mL for DPPH solutions) compared to respective ligands. The interaction study of compounds (1 s4 s) to DNA and BSA showed prominent binding affinity.

中文翻译:

硒N-杂环碳加合物的生物活性和DNA / BSA相互作用

随着有机硒化合物在生物医学领域的应用前景广阔,目前的工作计划是合成硒加合物(1 s -4 s)及其各自的偶氮配体(1 a - 4 a),随后通过各种分析和鉴定方法进行鉴定。光谱技术,例如微量分析,紫外可见光,红外光谱,1 H和13 C NMR和电喷雾电离质谱(ESI-MS)。此外,使用体外方法测试了合成化合物的生物潜力,例如抗氧化剂,抗菌剂,溶血性,DNA和牛血清白蛋白(BSA)相互作用,稳定性和亲脂性楷模。在研究的12-68小时内,所有化合物均以溶液形式稳定,并且在logP 0.66-0.85的范围内显示出良好的亲脂性。在生物学活性方面,硒化合物在0.3 mg / mL的浓度下均表现出更好的抗微生物作用(对金黄色葡萄球菌的抗药性为17.4±0.5–25.3±0.8 mm,对大肠杆菌的抗微生物性为18.6±0.7–24.1±0.9 )和抗氧化剂与各自的配体相比,电位(IC 50为DPPH溶液为40.0-62.0μg/ mL)。化合物(1 s4 s)与DNA和BSA的相互作用研究显示出显着的结合亲和力。
更新日期:2020-09-16
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