Preparation and characterization of Gum Arabic Schiff's bases based on 9-aminoacridine with in vitro evaluation of their antimicrobial and antitumor potentiality.

Autor: El-Sayed NS; Cellulose & Paper Department, National Research Centre, 33 El-Bohouth St. Former (El-Tahrir St.), Dokki, Giza, P.O. 12622, Egypt., Hashem AH; Botany and Microbiology Department, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt. Electronic address: amr.hosny86@azhar.edu.eg., Kamel S; Cellulose & Paper Department, National Research Centre, 33 El-Bohouth St. Former (El-Tahrir St.), Dokki, Giza, P.O. 12622, Egypt. Electronic address: samirki@yahoo.com.
Jazyk: angličtina
Zdroj: Carbohydrate polymers [Carbohydr Polym] 2022 Feb 01; Vol. 277, pp. 118823. Date of Electronic Publication: 2021 Oct 29.
DOI: 10.1016/j.carbpol.2021.118823
Abstrakt: The conjugation between drug and biopolymers through an easily hydrolysable bond such as ester linkage, disulfide linkage, or imine-bond have been extensively employed to control the drug release pattern and improve its bioavailability. This work described the conjugation of 9-aminoacridine (9-AA) to Gum Arabic (GA) via Schiff's base, as a pH-responsive bond. First, GA was oxidized to Arabic Gum dialdehyde (AGDA), then a different amount of 9-AA (10, 25, and 50 mg 9-AA) was coupled to defined amount of AGDA, the coupling was confirmed by elemental analysis and different spectroscopic tools. In addition, the physical features of Schiff's base conjugates including surface morphology, thermal stability, and crystalline structure were examined. The thermogravimetric analysis revealed that the incorporation of 9-AA slightly improved the thermal stability. The coupling of 9-AA to AGDA dramatically enhanced its in vitro antimicrobial and antitumor activities. All conjugates exhibited broad-spectrum activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, and Candida albicans. Moreover, AGA 25 and AGA 50 demonstrated promising capability to suppress the proliferation of human colon cancer cell line (Caco-2), with IC 50 190.10 and 180.80 μg/mL respectively.
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Databáze: MEDLINE