Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs

• Published in: Biomolecules (Basel, Switzerland) Vol. 11; no. 11; p. 1568
• Main Authors: Abd-El-Aziz, Alaa S, Benaaisha, Maysun R, Abdelghani, Amani A, Bissessur, Rabin, Abdel-Rahman, Laila H, Fayez, Ahmed M, El-Ezz, Doaa Abou
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 22-10-2021; MDPI
• Subjects: Animals; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; Anti-inflammatory agents; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - pharmacology; anticancer activity; Antimicrobial activity; Antimicrobial agents; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antitumor activity; Antitumor agents; Aspirin; Aspirin - chemistry; Aspirin - pharmacology; Bacteria; Bioavailability; Biological activity; Breast cancer; Cell Survival - drug effects; Cell viability; Chemicals; dendrimer; Dendrimers - chemistry; Dendrimers - pharmacology; Doxorubicin; Drug delivery; Drug delivery systems; Drugs; E coli; Electrodes; Fourier transforms; gastrointestinal toxicity; Gentamicin; Gram-negative bacteria; Gram-positive bacteria; HEK293 Cells; Hep G2 Cells; Humans; in vivo and in vitro anti-inflammatory activity; Inflammation; MCF-7 Cells; Microbial Sensitivity Tests; Microorganisms; Scanning electron microscopy; Solvents; Toxicity; Tumor cell lines; aspirin; gastrointestinal toxicity; anticancer activity; in vivo and in vitro anti-inflammatory activity; dendrimer
• ISSN: 2218-273X; 2218-273X
• DOI: 10.3390/biom11111568

Designing nanocarriers with actions directed at a specific organ or tissue is a very promising strategy since it can significantly reduce the toxicity of a bioactive drug. In this study, an organometallic dendrimer was used to synthesize a biocompatible drug delivery system by attaching aspirin to the periphery of the dendrimer. Our goal is to enhance the bioavailability and anticancer activity of aspirin and reduce its toxicity through successive generations of organoiron dendrimers. The biological activity of aspirin-based dendrimer complexes was evaluated. The result of antimicrobial activity of the synthesized dendrimers also demonstrated an increase in their antimicrobial activity with increased generation of the dendrimers for most types of microorganisms. This study reveals for the first time that organoiron dendrimers linked with aspirin exhibit an excellent Gram-negative activity comparable to the reference drug Gentamicin. All synthesized dendrimers were tested for their anticancer activity against breast cancer cell lines (MCF-7), hepatocellular cell lines (Hep-G2), and a non-cancer cell line, Human Embryonic Kidney (HEK293), using the MTT cell viability assay and compared against a standard anticancer drug, Doxorubicin. Compounds
and
exhibited noticeable activity against both cell lines, both of which were more effective than aspirin itself. In addition, the in vivo anti-inflammatory activity and histopathology of swollen paws showed that the designed aspirin-based dendrimers displayed significant anti-inflammatory activity; however,
showed the best anti-inflammatory activity, which was more potent than the reference drug aspirin during the same period. Moreover, the coupling of aspirin to the periphery of organoiron dendrimers showed a significant reduction in the toxicity of aspirin on the stomach.