Preparation and characterization of Gum Arabic Schiff's bases based on 9-aminoacridine with in vitro evaluation of their antimicrobial and antitumor potentiality.
Aminacrine
/ chemical synthesis
Anti-Bacterial Agents
/ chemical synthesis
Antineoplastic Agents, Phytogenic
/ chemical synthesis
Bacillus subtilis
/ drug effects
Caco-2 Cells
Candida albicans
/ drug effects
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Escherichia coli
/ drug effects
Humans
Microbial Sensitivity Tests
Molecular Structure
Pseudomonas aeruginosa
/ drug effects
Schiff Bases
/ chemical synthesis
Staphylococcus aureus
/ drug effects
Structure-Activity Relationship
9-Aminoacridine
Antimicrobial activity
Antitumor activity
Gum Arabic
Imine linkage
Journal
Carbohydrate polymers
ISSN: 1879-1344
Titre abrégé: Carbohydr Polym
Pays: England
ID NLM: 8307156
Informations de publication
Date de publication:
01 Feb 2022
01 Feb 2022
Historique:
received:
06
09
2021
revised:
12
10
2021
accepted:
25
10
2021
entrez:
11
12
2021
pubmed:
12
12
2021
medline:
16
3
2022
Statut:
ppublish
Résumé
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
Identifiants
pubmed: 34893240
pii: S0144-8617(21)01210-8
doi: 10.1016/j.carbpol.2021.118823
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Antineoplastic Agents, Phytogenic
0
Schiff Bases
0
Aminacrine
78OY3Z0P7Z
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
118823Informations de copyright
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