Aramesh-Boroujeni Zahra, Jahani Shohreh, Khorasani-Motlagh Mozhgan, Kerman Kagan, Noroozifar Meissam
Isfahan University of Medical Sciences, Isfahan, Iran; Department of Chemistry, University of Sistan and Baluchestan, Zahedan, 98135-674, Iran.
Nano Bioeletrochemistry Research Center, Bam University of Medical Sciences, Bam, Iran.
J Trace Elem Med Biol. 2020 Sep;61:126564. doi: 10.1016/j.jtemb.2020.126564. Epub 2020 May 21.
There is a crucial need for finding and developing new compounds as the anticancer and antimicrobial agents with better activity, specific target, and less toxic side effects.
Base on the potential anticancer properties of lanthanide complexes, in the paper, the biological applications of terbium (Tb) complex, containing 2,9-dimethyl- 1,10-phenanthroline (MePhen) such as anticancer, antimicrobial, DNA cleavage ability, the interaction with FS-DNA (Fish-Salmon DNA) and BSA (Bovine Serum Albumin) was examined.
The interaction of Tb-complex with BSA and DNA was studied by emission spectroscopy, absorption titration, viscosity measurement, CD spectroscopy, competitive experiments, and docking calculation. Also, the ability of this complex to cleave DNA was reported by gel electrophoresis. Tb-complex was concurrently screened for its antibacterial activities by different methods. Besides, the nanocarriers of Tb-complex (lipid nanoencapsulation (LNEP) and the starch nanoencapsulation (SNEP)), as active anticancer candidates, were prepared. MTT technique was applied to measure the antitumor properties of these compounds on human cancer cell lines.
The experimental and docking results suggest significant binding between DNA as well as BSA with terbium-complex. Besides, groove binding plays the main role in the binding of this compound with DNA and BSA. The competitive experiment with hemin demonstrated that the terbium complex was bound at site III of BSA, which was confirmed by the docking study. Also, Tb-complex was concurrently screened for its DNA cleavage, antimicrobial, and anticancer activities. The anticancer properties of LNEP and SNEP are more than the terbium compound.
Tb-complex can bond to DNA/BSA with high binding affinity. Base on biological applications of Tb-complex, it can be concluded that this complex and its nanocarriers can suggest as novel anticancer, antimicrobial candidates.
迫切需要寻找和开发新的化合物作为具有更好活性、特定靶点和更低毒副作用的抗癌和抗菌药物。
基于镧系元素配合物的潜在抗癌特性,本文研究了含2,9-二甲基-1,10-菲啰啉(MePhen)的铽(Tb)配合物的生物学应用,如抗癌、抗菌、DNA切割能力、与FS-DNA(鱼-鲑鱼DNA)和BSA(牛血清白蛋白)的相互作用。
通过发射光谱、吸收滴定、粘度测量、圆二色光谱、竞争实验和对接计算研究了Tb配合物与BSA和DNA的相互作用。此外,通过凝胶电泳报道了该配合物切割DNA的能力。采用不同方法同时筛选Tb配合物的抗菌活性。此外,制备了Tb配合物的纳米载体(脂质纳米包封(LNEP)和淀粉纳米包封(SNEP))作为活性抗癌候选物。应用MTT技术测定这些化合物对人癌细胞系的抗肿瘤特性。
实验和对接结果表明DNA以及BSA与铽配合物之间存在显著结合。此外,沟槽结合在该化合物与DNA和BSA的结合中起主要作用。与血红素的竞争实验表明铽配合物结合在BSA的位点III,对接研究证实了这一点。此外,同时筛选了Tb配合物的DNA切割、抗菌和抗癌活性。LNEP和SNEP的抗癌特性优于铽化合物。
Tb配合物能以高结合亲和力与DNA/BSA结合。基于Tb配合物的生物学应用,可以得出结论,该配合物及其纳米载体可作为新型抗癌、抗菌候选物。