Department of Chemistry, University of Prince Edward Island, 550 University Avenue, Charlottetown, PE, C1A 4P3, Canada.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA University), Giza, 12566, Egypt.
Macromol Biosci. 2021 Jan;21(1):e2000242. doi: 10.1002/mabi.202000242. Epub 2020 Oct 15.
The synthesis of a novel and attractive class of nonsteroidal anti-inflammatory and antimicrobial organoiron dendrimers attached to the well-known drug ibuprofen is achieved. The structures of these dendrimers are established by spectroscopic and analytical techniques. The antimicrobial activity of these dendrimers is investigated and tested against five human pathogenic Gram-positive and Gram-negative bacteria, and minimum inhibitory concentrations are reported. Some of these synthesized dendrimers exhibit higher inhibitory activity against methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Staphylococcus warneri compare to the reference drugs. As well, the in vitro and in vivo anti-inflammatory activities of these dendrimers are evaluated. The results of in vivo anti-inflammatory activity and histopathology of inflamed paws show that all dendrimers display considerable anti-inflammatory activity; however, second-generation dendrimer (G2-D6) shows the best anti-inflammatory activity, which is more potent than the commercial drug ibuprofen at the same tested dose. Results of the toxicity study reveal that G2-D6 is the safest drug on biological tissues.
合成了一类新型的、有吸引力的非甾体抗炎和抗菌有机铁树状大分子,这些分子连接在著名药物布洛芬上。这些树状大分子的结构通过光谱和分析技术确定。研究了这些树状大分子的抗菌活性,并对五种人体致病的革兰氏阳性和革兰氏阴性菌进行了测试,报告了最小抑菌浓度。与参比药物相比,一些合成的树状大分子对耐甲氧西林金黄色葡萄球菌、万古霉素耐药粪肠球菌和华纳葡萄球菌具有更高的抑制活性。此外,还评估了这些树状大分子的体外和体内抗炎活性。体内抗炎活性和发炎爪子的组织病理学研究结果表明,所有树状大分子都表现出相当强的抗炎活性;然而,第二代树状大分子(G2-D6)表现出最好的抗炎活性,在相同测试剂量下比商业药物布洛芬更有效。毒性研究结果表明,G2-D6 对生物组织是最安全的药物。