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

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 t...

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Main Authors:	Alaa S. Abd-El-Aziz, Maysun R. Benaaisha, Amani A. Abdelghani, Rabin Bissessur, Laila H. Abdel-Rahman, Ahmed M. Fayez, Doaa Abou El-ezz
Format:	article
Language:	EN
Published:	MDPI AG 2021
Subjects:	dendrimer aspirin in vivo and in vitro anti-inflammatory activity anticancer activity gastrointestinal toxicity Microbiology QR1-502
Online Access:	https://doaj.org/article/703d4dd347ec4aa8bae39315562fcb2f
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spelling	oai:doaj.org-article:703d4dd347ec4aa8bae39315562fcb2f2021-11-25T16:51:57ZAspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs10.3390/biom111115682218-273Xhttps://doaj.org/article/703d4dd347ec4aa8bae39315562fcb2f2021-10-01T00:00:00Zhttps://www.mdpi.com/2218-273X/11/11/1568https://doaj.org/toc/2218-273XDesigning 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 <b>G3-D9-Asp</b> and <b>G4-D12-Asp</b> 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, <b>G2-D6-Asp</b> 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.Alaa S. Abd-El-AzizMaysun R. BenaaishaAmani A. AbdelghaniRabin BissessurLaila H. Abdel-RahmanAhmed M. FayezDoaa Abou El-ezzMDPI AGarticledendrimeraspirinin vivo and in vitro anti-inflammatory activityanticancer activitygastrointestinal toxicityMicrobiologyQR1-502ENBiomolecules, Vol 11, Iss 1568, p 1568 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	dendrimer aspirin in vivo and in vitro anti-inflammatory activity anticancer activity gastrointestinal toxicity Microbiology QR1-502
spellingShingle	dendrimer aspirin in vivo and in vitro anti-inflammatory activity anticancer activity gastrointestinal toxicity Microbiology QR1-502 Alaa S. Abd-El-Aziz Maysun R. Benaaisha Amani A. Abdelghani Rabin Bissessur Laila H. Abdel-Rahman Ahmed M. Fayez Doaa Abou El-ezz Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
description	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 <b>G3-D9-Asp</b> and <b>G4-D12-Asp</b> 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, <b>G2-D6-Asp</b> 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.
format	article
author	Alaa S. Abd-El-Aziz Maysun R. Benaaisha Amani A. Abdelghani Rabin Bissessur Laila H. Abdel-Rahman Ahmed M. Fayez Doaa Abou El-ezz
author_facet	Alaa S. Abd-El-Aziz Maysun R. Benaaisha Amani A. Abdelghani Rabin Bissessur Laila H. Abdel-Rahman Ahmed M. Fayez Doaa Abou El-ezz
author_sort	Alaa S. Abd-El-Aziz
title	Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
title_short	Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
title_full	Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
title_fullStr	Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
title_full_unstemmed	Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs
title_sort	aspirin-based organoiron dendrimers as promising anti-inflammatory, anticancer, and antimicrobial drugs
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/703d4dd347ec4aa8bae39315562fcb2f
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Aspirin-Based Organoiron Dendrimers as Promising Anti-Inflammatory, Anticancer, and Antimicrobial Drugs

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