The Differential Tissue Distribution of the Citrus Flavanone Naringenin Following Gastric Instillation

Citrus flavonoids have been investigated for their biological activity, with both anti-inflammatory and -carcinogenic effects being reported. However, little information is known on the bioavailability of these compounds in vivo. The objectives of this study were to determine the tissue distribution of naringenin after gastric gavage of [³H]-naringenin to rats. Unlabelled naringenin was also used to quantify the levels of naringenin and its major metabolites in tissues and eliminated in the urine and faeces. Significant radioactivity was detected in the plasma as well as all tissues examined 2?h post-gavage. After 18?h, higher levels of radioactivity were retained in plasma and tissues (55% of the administered radioactivity). Investigation of the nature of metabolites, using unlabelled naringenin, revealed that the glucuronides were the major components in plasma, tissues and urine, in addition to the colonic metabolite 3-(4-hydroxyphenyl) propionic acid, detected in the urine. The aglycone was the form extensively retained in tissues after 18?h post-gavage. Total identified metabolites detected after 18?h in most tissues were only 1–5% of the levels detected after 2?h. However, the brain, lungs and heart retained 27, 20 and 11%, respectively, relative to the total metabolites detected at 2?h. While radioactive detection suggests increased levels of breakdown products of naringenin after 18?h versus 2?h, the products identified using unlabelled naringenin are not consistent with this, suggesting that a predominant proportion of the naringenin breakdown products at 18?h are retained as smaller decomposition molecules which cannot yet be identified.     

Synthesis,anti-inflammatory,cytotoxic, and COX-1/2 inhibitory activities of cyclic imides bearing 3-benzenesulfonamide,oxime, and β-phenylalanine scaffolds: a molecular docking study

Abstract

Cyclic imides containing 3-benzenesulfonamide, oxime, and β-phenylalanine derivatives were synthesised and evaluated to elucidate their in vivo anti-inflammatory and ulcerogenic activity and in vitro cytotoxic effects. Most active anti-inflammatory agents were subjected to in vitro COX-1/2 inhibition assay. 3-Benzenesulfonamides (2–4, and 9), oximes (11–13), and β-phenylalanine derivative (18) showed potential anti-inflammatory activities with 71.2–82.9% oedema inhibition relative to celecoxib and diclofenac (85.6 and 83.4%, respectively). Most active cyclic imides 4, 9, 12, 13, and 18 possessed ED₅₀ of 35.4–45.3?mg kg^?1 relative to that of celecoxib (34.1?mg kg^?1). For the cytotoxic evaluation, the selected derivatives 2–6 and 8 exhibited weak positive cytotoxic effects (PCE = 2/59–5/59) at 10?μM compared to the standard drug, imatinib (PCE = 20/59). Cyclic imides bearing 3-benzenesulfonamide (2–5, and 9), acetophenone oxime (11–14, 18, and 19) exhibited high selectivity against COX-2 with SI > 55.6–333.3 relative to that for celecoxib [SI > 387.6]. β-Phenylalanine derivatives 21–24 and 28 were non-selective towards COX-1/2 isozymes as indicated by their SI of 0.46–0.68.     

Novel Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and Other Coronaviruses: A Genome-wide Comparative Annotation and Analysis

Molecular and Cellular Biochemistry - Novel strain of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) causes mild to severe respiratory illness. The early symptoms may be fever, dry...     

Green synthesis,characterization, enhanced functionality and biological evaluation of silver nanoparticles based on Coriander sativum

The present study focused on the green synthesis of silver nanoparticles from Coriander sativum (CS) containing structural polymers, phenolic compounds and glycosidic bioactive macromolecules. Plant phenolic compounds can act as antioxidants, lignin, and attractants like flavonoids and carotenoids. Henceforth, silver nanoparticles (AgNPs) were prepared extracellularly by the combinatorial action of stabilizing and reduction of the CS leaf extract. The biologically synthesized CS-AgNPs were studied by UV-spectroscopy, zeta potential determination, scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analysis to characterize and confirm the formation of crystalline nanoparticles. The synthesized nanoparticles demonstrated strong antimicrobial activity against all microbial strains examined with varying degrees. The scavenging action on free radicals by CS-AgNPs showed strong antioxidant efficiency with superoxide and hydroxyl radicals at different concentrations as compared with standard ascorbic acid. The presence of in vitro anticancer effect was confirmed at different concentrations on the MCF-7 cell line as revealed with decrease in cell viability which was proportionately related to the concentration of CS-AgNPs illustrating the toxigenic nature of synthesized nanoparticles on cancerous cells.     

Molecular identification of Campanulotes bidentatus Scopoli, 1763 (Phthiraptera,Philopteridae) infecting the domestic pigeon Columba livia from Saudi Arabia

The taxonomy of the order Phthiraptera is unstable and still problematic to researchers. Most of the current taxon classifications are mainly based on morphological features. Campanulotes bidentatus belongs to the chewing lice of the Philopteridae family that mostly parasitic on birds. There is a lack of sequence data and phylogenetic analyses on the family Philopteridae. In the current study, C. bidentatus was collected from the domestic pigeon Columba livia and identified morphologically and molecularly based on the mitochondrial cytochrome c oxidase subunit 1 gene (COI). The infection rate of the Campanulotes genus was approximately 58.82% in this study. Phylogenetic analysis based on the mt COI gene was informative for members of Philopteridae and the group taxon genera formed distinct clades. Future studies were recommended using the 16s rRNA to enhance the tree topology and obtain clear differentiation between genera.     

Effects of nonsteroidal ecdysone agonist RH-5992 and chitin biosynthesis inhibitor lufenuron on <Emphasis Type="Italic">Spodoptera littoralis</Emphasis> (Boisduval, 1833)

Comparative studies of the effects of two compounds, tebufenozide (an ecdysone agonist) and lufenuron (an insect growth regulator inhibiting chitin synthesis), were conducted on Spodoptera littoralis (Boisduval, 1833). The compounds, orally administered, caused larval mortality proportional to the concentrations in the food source. Tebufenozide initiated precocious molting, and lufenuron, and inhibited chitin synthesis. In both cases, larvae were unable to complete the molting process and died in the old larval cuticle. Larvae contaminated by sublethal doses completed their development to adulthood. Lufenuron is more active than is tebufenozide. LD-50 for lufenuron is 0.0001ppm and for tebufenozide 0.001ppm. Topical application of the test compounds to eggs caused dose- and agedependent inhibition of embryonic development. Application of tebufenozide in the second half of embryogenesis caused precocious molting of eclosed larvae of the 1^st instar. Some morphological changes in the process of larval-pupal transformation were also observed. Tested compounds also reduced reproduction in adult individuals that had been treated by the tested compounds in the larval stage.     

Performance of diagnostic biomarkers in predicting liver fibrosis among hepatitis C virus-infected Egyptian children

The aim of the present study was to identify specific markers that mirror liver fibrosis progression as an alternative to biopsy when biopsy is contraindicated, especially in children. After liver biopsies were performed, serum samples from 30 hepatitis C virus (HCV) paediatric patients (8-14 years) were analysed and compared with samples from 30 healthy subjects. All subjects were tested for the presence of serum anti-HCV antibodies. Direct biomarkers for liver fibrosis, including transforming growth factor-β1, tissue inhibitor of matrix metalloproteinase-1 (TIMP-1), hyaluronic acid (HA), procollagen type III amino-terminal peptide (PIIINP) and osteopontin (OPN), were measured. The indirect biomarkers aspartate and alanine aminotransferases, albumin and bilirubin were also tested. The results revealed a significant increase in the serum marker levels in HCV-infected children compared with the healthy group, whereas albumin levels exhibited a significant decrease. Significantly higher levels of PIIINP, TIMP-1, OPN and HA were detected in HCV-infected children with moderate to severe fibrosis compared with children with mild fibrosis (p < 0.05). The diagnostic accuracy of these direct biomarkers, represented by sensitivity, specificity and positive predictive value, emphasises the utility of PIIINP, TIMP-1, OPN and HA as indicators of liver fibrosis among HCV-infected children.     

Effectiveness of entomopathogenic nematodes Steinernema feltiae and Heterorhabditis bacteriophora on the Colorado potato beetle Leptinotarsa decemlineata (Say) (Coleoptera: Chrysomelidae) under laboratory and greenhouse conditions

In laboratory and greenhouse studies, the invading ability, virulence, and mortality caused by Stinernema feltiae and Heterorhabditis bacteriophora were compared. After one and two days of exposure to either nematode species, the mortality of Colordo potato beetle (CPB) Leptinotarsa decemlineata larvae at different instars, third and fourth, was recorded and the number of nematodes invading cadavers was more than the number of nematodes inside the larvae at the late last instar (one day before pre-pupa). Two concentrations, 250 and 500 IJs/dish, infective juvenile nematodes/0.5 ml were tested on different CPB larval instar. S. feltiae was more effective, with fourth instar rather than third and late last instar. On the other hand, H. bacteriophora showed a very weak effect with L. decemlineata. Also it was clear that S. feltiae was more effective and faster than H. bacteriophora: more than 70% of larvae were killed within 24 hours compared with H. bacteriophora which killed 40% of larvae within 48–72 hours. A significant difference in invading efficiency was observed with concentration 2500 IJs/pot in the greenhouse test. The number of adult females found in the cadavers of L. decemlineata larvae was always higher than the number of males. Foliage application of S. feltiae and H. bacteriophora resulted in a significant reduction of the number of damaged leaves and a lower index of damage compared with that in the control. We conclude that S. feltiae has significant potential and can help in the management of the Colorado potato beetle.     

Accumulation and translocation of Cd metal and the Cd-induced production of glutathione and phytochelatins in <Emphasis Type="Italic">Vicia faba</Emphasis> L.

Translocation of cadmium (Cd) in the tissues of Vicia faba, the water content in biomass, the biomass production, and the glutathione and phytochelatin tissue concentrations were studied and correlated with the plant sensitivity and/or tolerance to Cd. The total concentrations of Cd were determined by inductively coupled plasma/mass spectrometry (ICP-MS), the concentrations of glutathione (GSH) and phytochelatins 2 and 3 (PC2 and PC3) were determined by on-line high performance liquid chromatography/electrospray-ionization tandem mass spectrometry (HPLC–ESI–MS–MS) in the roots and leaves of the sensitive and the tolerant cultivars of V. faba grown in Cd containing nutrient solutions (NS, 0–100 μmol l⁻¹ Cd²⁺). Both the cultivars of V. faba accumulate a major portion of Cd in the roots and only a minor part of ca. 4% in the leaves. The differences between the cultivars concerning Cd accumulation in leaves were apparent from higher Cd concentrations in NS and the Cd amount in the sensitive cultivar was approximately twice as high. In the roots, the differences between the cultivars in the Cd accumulation were only statistically significant with the highest Cd concentrations in NS, with the tolerant cultivar accumulating about 16% more of Cd compared to the sensitive one. The biomass production of the sensitive cultivar decreased approximately twice as fast with increasing Cd concentration in NS. The biomass water content decreased with increasing Cd concentration in NS in both the cultivars. In general, the GSH concentration did not linearly correlate with Cd accumulation, except for the roots of the sensitive cultivar where it was independent, and was higher in the sensitive cultivar than in the tolerant one in both the leaves and roots. The GSH concentration in leaves was approximately one order of magnitude higher than that in the roots for both the cultivars. The relationships between the PC and Cd concentrations in tissues were found nonlinear. At lower Cd accumulation levels, the PC concentrations followed an increase in the Cd accumulation in both the roots and leaves, whereas at higher Cd accumulations the relations differed between roots and leaves. In the roots, the PC concentrations decreased with increasing Cd accumulation, whereas the PC concentration in the leaves followed the decrease in the Cd accumulation.