新型异羟肟酸基有机硒杂化物的设计、合成及生物学评价

Design, Synthesis, and Biological Evaluation of Novel Hydroxamic Acid-Based Organoselenium Hybrids.

作者信息

Alotaibi Jameelah S, Al-Faiyz Yasair S, Shaaban Saad

机构信息

Chemistry Department, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.

Chemistry Department, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.

出版信息

Pharmaceuticals (Basel). 2023 Feb 28;16(3):367. doi: 10.3390/ph16030367.

We report the design and synthesis of novel hydroxamic acid-tethered organoselenium (OSe) hybrids. Their antimicrobial and anticancer activities were assessed against different microbes (e.g., (), (), and ()), as well as liver and breast carcinomas. OSe hybrid showed promising anticancer activity, with IC = 7.57 ± 0.5 µM against HepG2 and IC = 9.86 ± 0.7 µM against MCF-7 cells. Additionally, OSe compounds and exhibited promising antimicrobial activities, particularly against (IA% = 91.7 and 83.3) and (IA% = 90.5 and 71.4). The minimum inhibitory concentration (MIC) assay confirmed the potential antimicrobial activity of OSe compound . OSe compounds and displayed good antioxidant activities compared to vitamin C in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. These results indicate that hydroxamic acid-based organoselenium hybrids have promising biological activities such as anticancer, antimicrobial, and antioxidant properties, especially compounds , , and which warrant further studies.

我们报告了新型异羟肟酸连接的有机硒（OSe）杂化物的设计与合成。评估了它们对不同微生物（如大肠杆菌、金黄色葡萄球菌和白色念珠菌）以及肝癌和乳腺癌的抗菌和抗癌活性。OSe杂化物1对肝癌细胞HepG2显示出有前景的抗癌活性，其IC50 = 7.57 ± 0.5 μM，对MCF - 7细胞的IC50 = 9.86 ± 0.7 μM。此外，OSe化合物2和3表现出有前景的抗菌活性，尤其是对大肠杆菌（抑制率分别为91.7%和83.3%）和金黄色葡萄球菌（抑制率分别为90.5%和71.4%）。最低抑菌浓度（MIC）测定证实了OSe化合物3的潜在抗菌活性。在2,2 - 二苯基 - 1 - 苦基肼（DPPH）和2,2'- 偶氮二（3 - 乙基苯并噻唑啉 - 6 - 磺酸）（ABTS）测定中，与维生素C相比，OSe化合物2和3表现出良好的抗氧化活性。这些结果表明，基于异羟肟酸的有机硒杂化物具有有前景的生物活性，如抗癌、抗菌和抗氧化特性，尤其是化合物1、2、3和4值得进一步研究。