Recently, chemical modifications of chitosan (CS) have attracted the attention of scientific researchers due to its wide range of applications. In this research, chitin (CH) was extracted from the scales of Cyprinus carpio fish and converted to CS by three chemical steps: (i) demineralization, (ii) deprotonation, and (iii) deacetylation. The degree (measured as a percentage) of deacetylation (DD %) was calculated utilizing the acid–base titration method. The structure of CS was characterized by Fourier transform infrared (FT-IR) spectroscopy and thermogravimetric analysis (TGA). Three new CS Schiff bases (CSSBs) (CS-P1, CS-P2, and CS-P3) were synthesized via coupling of CS with 2-chloroquinoline-3-carbaldehyde, quinazoline-6-carbaldehyde, and oxazole-4-carbaldehyde, respectively. The newly prepared derivatives were verified, structurally, by nuclear magnetic resonance (1H and 13C NMR) and FT-IR spectroscopy. Antimicrobial activity was evaluated for the prepared compounds against both “Gram-negative” and “Gram-positive” bacteria, namely, Escherichia coli, Klebsiella pneumonia, Staphylococcus aureus, and Streptococcus mutans, in addition to two kinds of fungi, Candida albicans and Aspergillus fumigates. Cytotoxicity of the synthesized CSSBs was evaluated via a MTT screening test. The results indicated a critical activity increase of the synthesized compound rather than CS generally tested bacteria and fungi and the absence of cytotoxic activity. These findings suggested that these new CSSBs are novel biomaterial candidates with enhanced antibacterial and nontoxic characteristics for applications in areas of both biology and medicine.
5-fluorouracil (5-FU) is a specific anti-cancer agent that is generally used to treat gastrointestinal, colorectal, and breast cancer. In this work, chitosan (CS) was extracted from local fish scales using an established method. 5-FU was then converted to 1-acetic acid-5-fluorouracil (FUAC) and reacted with this CS to prepare chitosan-1-acetic acid-5-fluorouracil (CS-FUAC) conjugates as a colon-specific prodrug. All compounds were characterized by Proton nuclear magnetic resonance (1H-NMR), Fourier-transform infrared (FTIR), and UV-visible spectroscopy. The synthesized compound was subjected to a chemical stability study in phosphate buffer (0.2 M, pH 7.4) and in KCl/HCl buffer (0.2 M, pH 1.2) at different time intervals (0–240 min) and incubation at 37 °C. This revealed a significantly greater stability and a longer half-life for the CS-FUAC than for FUAC. Hemolytic activity results indicated a much lower toxicity for CS-FUAC than for 5-FU and supported consideration of CS-FUAC for further biological screening and application trials. The percentage of FUAC in the conjugates was determined by subjecting the prodrug to treatment in basic media to hydrolyze the amide bond, followed by absorbency measurements at 273 nm. The cytotoxicity studies of the conjugates were also evaluated on human colorectal cancer cell line (HT-29), which showed that the conjugates are more cytotoxic than the free drug. Therefore, CS-FUAC conjugates can be considered to represent potential colon-specific drug delivery agents, with minimal undesirable side effects, for colon cancer therapy.
Methotrexate (MTX) is the most important drug used in the treatment of several kinds of cancers, such as colon cancer. However, this drug can cause a reduction in the target tissue bioavailability. It is administered orally and absorbed quickly. This study aimed to produce an anti-colon cancer prodrug based on MTX via loading it into a biopolymer compound. Chitosan (CS) was extracted from scales of local fish by utilizing a previously published protocol. The MTX was then transformed to Methotrexateimidazole and loaded into CS to prepare Chitosan -Methotrexate (CS-MTX) conjugates as colon cancer prodrugs. Fourier-transform infrared (FTIR), UV-visible spectroscopy, and 1 H-NMR were used to analyse the structure of the prepared compounds. The prepared compounds were also tested for hemolytic activity. Chemical stability was studied using 0.2 M from the different buffer types with a pH of 1.2 and 7.4 over different periods about 240 min and kept in an incubator at 37 C. The loading percentage was measured by hydrolysing the amide bond in basic media followed by the measurement of the absorbency at 273 nm. Three types of cancer cells, MCF-7, MDA-MB-231, and MDA-MB-453, were used to test the anticancer effects of CS-MTX by using tetrazolium bromide (MTT) assay. The results indicated that the viability of human breast cancer cell lines decreased because of the use of CS-MTX. This study also showed that CS-MTX was less toxic than the original drug. Therefore, it may be measured for additional biological analyses and medical applications. The results presented here showed that the new compound is remarkably stable in comparison with MTX and has longer half-life (t ½ ). Therefore, the CS-MTX has promising strategies through minimising the side effects of anti-colon tumour drugs.
Effect of Uracil's derivatives on enzyme glutamate oxaloacetate transaminase (GOT) for sample of normal human and some types of leukemia patients, acute lymphatic(ALL) (11 cases), acute mylosyticl (AML) (4 cases), acute mylomonocyticl (AMOL) (2cases), acute pro-mylocyticl (APL) (3 cases), chronic mylobid (CM) (4 cases) and chronic lymphatic (CLL) (4 cases) is investigated. The ages of patients are between (10-69 years). Some synthesized derivatives of uracil were used as an inhibitors and a comparison between the activity of (GOT) in the presence and absence of inhibitors for two-types of serums under the same conditions is studied. The percentage of inhibition and type of inhibition is also included in this study, which was showed degree of inhibitions in normal individuals between (31%-73%) and degree of inhibitions in patient's individuals between (25%-80%) which showed that inhibition was significantly higher in the sera of patient with leukemia. The activity was determined colorimetrically by Retiman and Frankel method.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.