Pharmacological Evaluation of Novel Organoiron Dendrimers as Antimicrobial and Anti‐Inflammatory Agents,Macromolecular Bioscience

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Pharmacological Evaluation of Novel Organoiron Dendrimers as Antimicrobial and Anti‐Inflammatory Agents
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-10-15 , DOI: 10.1002/mabi.202000242
Alaa S Abd-El-Aziz ₁ , Amani A Abdelghani ₁ , Ebtehal G El-Ghezlani ₁ , Doaa Abou El-Ezz ₂ , Laila H Abdel-Rahman ₃

Affiliation

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.

中文翻译：

新型有机铁树枝状聚合物作为抗菌和抗炎剂的药理学评价

合成了一类新颖且有吸引力的非甾体抗炎和抗微生物有机铁树枝状聚合物，该树枝状聚合物与众所周知的药物布洛芬相连。这些树枝状聚合物的结构是通过光谱和分析技术确定的。研究并测试了这些树枝状聚合物对五种人类致病性革兰氏阳性和革兰氏阴性细菌的抗菌活性，并报告了最低抑制浓度。其中一些合成的树枝状大分子对耐甲氧西林金黄色葡萄球菌、耐万古霉素屎肠球菌和华氏葡萄球菌表现出较高的抑制活性与参考药物比较。此外，还评估了这些树枝状聚合物的体外和体内抗炎活性。发炎爪的体内抗炎活性和组织病理学结果表明，所有树枝状聚合物都显示出相当大的抗炎活性；然而，第二代树枝状聚合物 ( G2-D6 ) 显示出最好的抗炎活性，在相同的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 是对生物组织最安全的药物。

更新日期：2020-10-15

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