Helminthiasis is a significant economic burden on grazing cattle. Increased resistance to currently available synthetic anthelmintics used to treat helminthiasis, and anthelmintic residues in meat and dairy products pose a significant worldwide health threat. These obstacles require the development of new anthelmintics capable of combating drug resistance while also exhibiting improved safety profiles. Rhynchosia cana (Fabaceae) is a herb that has historically been used as a worm expeller. To evaluate the phytochemical profile and explore the anti-oxidant and anthelmintic effects of different extracts of Rhynchosia cana (R. cana) by In silico and In vitro methods. Using standardised chemical tests as defined in the literature, phytochemical research was carried out. Using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Hydrogen peroxide (H2O2) radicals scavenging assay, In vitro free radical scavenging behaviour of different extracts was quantitatively estimated, whereas In-vitro anthelmintic activity was measured against Pheretima posthuma (P. posthuma) (Annelida). The molecular docking analysis was then carried out to establish compounds with good efficiency for anti-oxidant activity against the catalase, superoxide dismutase, glutathione-S-transferase, glutathione reductase, glutathione peroxidase and tubulin-colchicine enzyme for anthelmintic activity. Furthermore, ADME/T profiles have been tested by ADMET SAR. The various extracts of R cana potentially inhibited the reactive oxygen species (ROS) and possessed anti-oxidant activity. In anti-oxidant assays, the IC50 values ranged from 62.08 to 440.08 μg/mL for PERC, EARC, and MERC. All the extracts demonstrated anthelmintic behaviour on P. posthuma that was dose-dependent and statistically relevant. On the other side, molecular docking analysis reveals that Gallocatechin has the best fitness score of -7.1 kcal/mol with tubulin-colchicine enzyme; Rhynchosin, Luteolin-3',4'-dimethyl ether, Isoorientin and Orientin has the best fitness scores with different targets related to the oxidation process. In addition, all compounds were in the array of expected properties to fulfil the Lipinski law of five to be accepted as drug-like potential. The observation indicates that the R. cana possesses anti-oxidant and anthelmintic activity In vitro and In silico assays. However, further research was needed to elucidate their primary molecular mechanism of action, safety, toxicity, and bioavailability.
Mushrooms have bioactive compounds that have antimicrobial, anti-cancer and antioxidant activities among other medicinal benefits. In the present study, we examined the anti-cell proliferation activities of mushrooms from eight genera obtained from the wild in Nigeria. Saccharomyces cerevisiae was used as a model organism to screen mushroom extracts for anti-cell proliferation activity. Polyphenols, high molecular weight polysaccharides and low molecular weight compounds from aqueous extracts were obtained from the test mushrooms using methanol and water respectively. The extracts were screened in vitro at different concentrations of extracts with the CyQuant cell proliferation assay. The high molecular
... Show More1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.
To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.
The designed compounds were synthesized using convent
The research study included the synthesis of a new series of heterocyclic derivatives containing the antibiotic Levofloxacin. The first way provides for the reaction of Levofloxacin with thionyl chloride in benzene as a solvent to give an acid chloride derivative. A new class of acid hydrazide synthesized from Levofloxacin was studied. Schiff bases were produced via the reaction of acid hydrazide with substituted aromatic ketones in methanol. The next stage involved the response of Schiff bases with thioglycolic acid and mono chloroacetic acid in DMF to produce derivatives of the antibiotic levofloxacin that have five heterocyclic members, including the derivatives thiazolidine-4-one and oxazolidine-5-one. The FTIR, 1HNMR, a
... Show MoreMetal oxide nanocomposites (MONCs) manufacturing is increasingly gaining popularity. The primary cause of this is the broad range of applications for such materials, which include fuel cells, photovoltaics, cosmetics, medicine, semiconductor packing materials, water treatment, and catalysts. Due to their size, stability, high surface area, catalytic activity, simplicity in fabrication, and selectivity for particular reactions. The MONCs with various morphologies have been created by physical, chemical, and biological processes, such as sol-gel, hydrothermal, co-precipitation, solvothermal, and microwave irradiation. Eugenol (4-allyl-2-methoxyphenol) is a major component of clove essential oil and it was found in various plant groups, has
... Show MoreAllosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.
A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR
Crabs belong to the crustacean family (Decapods crustacean), and their shells contain natural ingredients from which the bioactive compounds are derived. It has been used as folklore medicine in cancer treatment. We investigate the possible anti-inflammatory and anti-oxidant effects for crab shells and whole crabs. Thirty-six rats (150–200 gm) from both sexes were used, divided into six groups, the anti-inflammatory and anti-oxidant activity measured using cotton pellet induce granuloma model. Detection of tumor necrosis factor alpha (TNF α), Interleukin 1 beta (IL-1β), superoxide (SOD), and malondialdehyde (MDA) levels using ELISA Kits. The data analysis by one-way ANOVA followed by the Tukey test. Values are significant at (p < 0.05).
... Show MorePower-electronic converters are essential elements for the effective interconnection of renewable energy sources to the power grid, as well as to include energy storage units, vehicle charging stations, microgrids, etc. Converter models that provide an accurate representation of their wideband operation and interconnection with other active and passive grid components and systems are necessary for reliable steady state and transient analyses during normal or abnormal grid operating conditions. This paper introduces two Laplace domain-based approaches to model buck and boost DC-DC converters for electromagnetic transient studies. The first approach is an analytical one, where the converter is represented by a two-port admittance model via mo
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