The flavonoglycone hesperidin is recognized as a potent anti-inflammatory, anticancer, and antioxidant agent. However, its poor bioavailability is a crucial bottleneck regarding its therapeutic activity. Gold nanoparticles are widely used in drug delivery because of its unique properties that differ from bulk metal. Hesperidin loaded gold nanoparticles were successfully prepared to enhance its stability and bioactive potential, as well as to minimize the problems associated with its absorption. The free radical scavenging activities of hesperidin, gold nanoparticles, and hesperidin loaded gold nanoparticles were compared with that of Vitamin C and subsequently evaluated in vitro using 2,2-diphenyl-1-picrylhydrazyl assay. The antioxidant pharmacophore-based structure-activity relationship analysis was assessed by the density functional theory as well as quantum chemical calculations. Moreover, the structural properties were utilized using Becke’s three-parameter hybrid exchange and Lee-Yang-Parr’s correction of functional approaches. Hesperidin-loaded gold nanoparticles were found to decrease hydrogen peroxide (H2O2) and thus induce Deoxyribonucleic acid (DNA) instability. In addition, hesperidin-gold nanoparticles were observed to display important antioxidant potential as well as ameliorate the functional activity of macrophages against
The synthesis oxadiazole derivative 2,5-disubstituted-1,3,4oxadiazole (3a,3b,3c) was prepared from reaction of N-(4-amino benzene sulphonyl)Morpholipebut-2-enehydrazide with (4-hydroxybenzaldehyde,4-methoxy benzaldehyde,4-ethoxybenzaldehyde) in the presence of lone as catalyst. The structure of (3a,3b,3c) was characterized by using FT-IR, H-NMR and spectroscopy. Nanoparticles of the prepared compounds have been fabricated in aqueous media using re-precipitation method.Characterization of the nano particles (ONPs) have been performed by using UV-VIS spectrophotometer and scanning electron micro scope ( SEM). The size of the nanoparticales were around 150-200 nm as indicated by (SEM). T
Human serum albumin (HSA) nanoparticles have been widely used as versatile drug delivery systems for improving the efficiency and pharmaceutical properties of drugs. The present study aimed to design HSA nanoparticle encapsulated with the hydrophobic anticancer pyridine derivative (2-((2-([1,1'-biphenyl]-4-yl)imidazo[1,2-a]pyrimidin-3-yl)methylene)hydrazine-1-carbothioamide (BIPHC)). The synthesis of HSA-BIPHC nanoparticles was achieved using a desolvation process. Atomic force microscopy (AFM) analysis showed the average size of HSA-BIPHC nanoparticles was 80.21 nm. The percentages of entrapment efficacy, loading capacity and production yield were 98.11%, 9.77% and 91.29%, respectively. An In vitro release study revealed that HSA-BIPHC nan
... Show MoreThe biological activities of some ternary nickel complexes with a Schiff base obtained from 4-dimethylaminobenzaldehyde and 2-aminophenol have been reported. The Schiff base ( HL1) acts as a primary ligand whereas, anthranilic acid ( HL2), 2-nitroaniline ( HL3), alanine ( HL4) and histidine ( HL5) act as secondary ligand or co-ligand. The anticancer activity of these compounds was studied against human colon carcinoma (HCT-116), human hepatocellular liver carcinoma (HEPG-2) and human breast carcinoma (MCF-7) cell lines. As per the results, the compounds were active against the cell lines. The antioxidant activity of the same compounds was evaluated using DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical scavenging and compared with ascorbic aci
... Show MoreAbstract: Colloidal gold nanoparticles (ringworm Palm or in the form of paper willow) have been prepared from HAuCl4 containing aqueous solution by hot chemical reduction method. The colloidal gold nanoparticles were characterized by SEM, EDX, and UV-VIS absorption spectroscopy. It was found that the variation of reduction time from boiling point affects the size of the nanoparticles and also in chemical reduction approach the size of nanoparticles can be controlled by varying the amount of variation the volume of reductant material with respect to the volume of HAuCL4.
A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50
... Show MoreBacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used
... Show MoreCitrus fruit contain variety of flavonoids such as Hesperidin (the principal flavonoid in oranges and grapefruit). Hesperidin is found in high concentration in fruit peel of oranges and in substantially lower concentration in juice of these fruits. Hesperidin was extracted from oranges peel by treating the peels with calcium hydroxide. HPLC technique was used to determine hesperidin. Hesperidin was saperated and purified in a purity of about 90.1-95.7% and yield about 1.5 %w/w from oranges peel dry powder. Both hesperidin and oranges peel extract showed significan antibacterial activity. Sensitivity to hesperidin and oranges peel extracts were not similar for the chosen bacteriaCrude orange peel extract gave a various antimicro
... Show MoreIn fish, a complex set of mechanisms deal with environmental stresses including hypoxia. In order to probe the hypothesis that hypoxia-induced stress could be manifested in varieties of pathways, a model species, mirror carp (Cyprinus carpio), were chronically exposed to hypoxic condition (dissolved oxygen level: 1.80±0.6mg/l) for 21 days and subsequently allowed to recover under normoxic condition (dissolved oxygen level: 8.2±0.5mg/l) for 7 days. At the end of these exposure periods, an integrated approach was applied to evaluate several endpoints at different levels of biological organisation. These included determination of (i) oxidative damage to DNA in erythrocytes (using modified comet assay), (ii) lipid peroxidation in liver sample
... Show MoreDiazotization reaction between 1-(2,4,6-Trihydroxy-phenyl)-ethanone and diazonium salts was carried out resulting in ligand 4-(3-Acetyl-2,4,6-trihydroxy-phenylazo)-N-(5-methyl-isoxazol-3-yl)-benzenesulfonamide, this in turn reacted with the next metal ions (V4+ , Cr3+ , Mn2+ and Cu2+) forming stable complexes with unique geometries such as (Octahedral for both Cr3+ , Mn2+ and Cu2+ ,squar pyramidal for V4+). The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible which proved the obtained geometries, fourier transfer proved the formation of azo group and and the coordination with metal ion through it. Pyrolysis (TGA & DSC) studies proved the coordination of water residues with me
... Show MoreEthanol as a solvent, a precursor of titanium isopropoxide and a stabilizer of either hydrochloric acid or ammonium hydroxide was used to prepare a titanium dioxide aqueous solution. The aqueous solutions with different values of pH and the morphology of the resultant reaction of the nanoparticles of titanium dioxide were investigated. The X-ray diffraction showed that at low temperatures and with acidic solutions, rutile structures are more favorable to grow on titanium dioxide synthesized, while at low and average temperatures and with base solutions, anatase phase is more pronounced. The crystalline form and the re-confirmation of the crystallite size growth were observed by the scanning electron microscopy. The atomi
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