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The protective and therapeutic anti-inflammatory and antioxidant potency of Malapterurus electricus (F. Malapteruridae) skin fish methanolic extract (FE) (300 mg/kg.b.wt/day for 7 days, orally) was tested in monosodium urate(MSU)-induced arthritic Wistar albino male rats' joints. Serum uric acid, TNF-α, IL-1β, NF-𝜅B, MDA, GSH, catalase, SOD, and glutathione reductase levels were all measured. According to the findings, FE significantly reduced uric acid levels and ankle swelling in both protective and therapeutic groups. Furthermore, it has anti-inflammatory effects by downregulating inflammatory cytokines, primarily through decreased oxidative stress and increased antioxidant status. All the aforementioned lesions were significantly improved in protected and treated rats with FE, according to histopathological findings. iNOS immunostaining revealed that protected and treated arthritic rats with FE had weak positive immune-reactive cells. Phytochemical analysis revealed that FE was high in fatty and amino acids. The most abundant compounds were vaccenic (24.52%), 9-octadecenoic (11.66%), palmitic (34.66%), stearic acids (14.63%), glycine (0.813 mg/100 mg), and alanine (1.645 mg/100 mg). Extensive molecular modelling and dynamics simulation experiments revealed that compound 4 has the potential to target and inhibit COX isoforms with a higher affinity for COX-2. As a result, we contend that FE could be a promising protective and therapeutic option for arthritis, aiding in the prevention and progression of this chronic inflammatory disease.

Premna odorata Blanco (Lamiaceae) is an ethnomedicinal plant native to different tropical regions. Although some reports addressed their anti-inflammatory, cytotoxic, and antituberculotic effects, their hepatoprotective potential is yet to be discovered. Accordingly, this study investigated the crude extract and different fractions of the plant leaves; metabolic profiling using liquid chromatography/high-resolution electrospray ionization mass spectroscopy (LC-HRESIMS) analysis, in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties for the dereplicated metabolite via online PreADMET program, ROS scavenger activity on the Hep G2 human liver cancer cell line, and the possible hepatic cellular treatment effects in alcohol-inflamed liver female Wistar albino rats. Metabolic profiling dereplicated a total of 28 metabolites from the crude extract and its various fractions. In silico ADMET and ROS scavenger activity screening suggested plant metabolites are of potential bioactivity. In vivo hepatic treatment with crude, defatted crude, and n-hexane leave extracts suggested all extracts significantly improved liver damage, which was indicated by the reduction of elevated serum levels of bilirubin, AST, ALT, ALP, CRP, TNF-α, ICAM-1, VCAM-1, and MDA. The reduced levels of GSH and TAC were normalized during the study. Histological examinations of liver tissue showed collagen fiber distribution nearly back to its normal pattern. The anti-inflammatory and antioxidant potentials of Premna odorata extracts could be partly related to the combined effects of these phytochemicals or their synergistic interactions.

The purpose of this study is to investigate the therapeutic efficacy of individual or combined doses of dehydro-epiandrosterone (DHEA) and quercetin in ameliorating some biochemical indices in liver of CuO-NPs intoxicated-rats. CuO-NPs (50 nm) was administered as a daily oral dose 100 mg/kg for 2 weeks to rats followed by the fore-mentioned antioxidants for 1 month. We highlighted the therapeutic effect of DHEA and quercetin against CuO-NPs toxicity through monitoring the alteration of liver enzyme activity, antioxidant defense mechanism, necrosis, apoptosis, histopathological alterations, and DNA damage. The rats given CuO-NPs only showed marked significant elevation in liver enzymes, alteration in oxidant-antioxidant balance and an elevation in the hepatic inflammatory marker; tumor necrosis factor-α. Additionally, over expression of both caspase-3 and Bax proteins were detected. Whereas, Bcl2 was down regulated and DNA fragmentation was elevated. Moreover, Histopathological examination of hepatic tissue reinforced the previous biochemical results. Co-treatment with either DHEA, quercetin alone or in combination ameliorated the deviated parameters with variable degrees against CuO-NPs toxicity in rat. In conclusion, our findings suggested that the aforementioned treatments exert therapeutic effect in CuO-NPs toxicity by diminishing oxidative stress, mRNA gene expression and hepatic tissues DNA damage.

Series of new sulfonylurea derivatives (gliclazide analogues) was synthesized and characterized. Thus, p-tolylsulfonylisocyanate was left to react with different amino derivatives under mild conditions to afford the desired sulfonylurea derivatives 1-5. The molecular structure of the compound N-(2,6-Dichlorophenylcarbamoyl)-4-methylbenzenesulfonamide, 1c has been elucidated by single crystal X-ray diffraction. Anti-diabetic properties of the synthesized compounds relative to anti-diabetic drug (gliclazidem MR60) were carried out, where most of the tested compounds showed significant activity for reducing the blood glucose level. The results revealed that compounds 1c and 5 showed better anti-diabetic activities compared with gliclazide. Activity of the most potent derivatives of sulfonylurea compounds namely 1c and 5 were increased using coated nanostructure tetraethyl orthosilicate (TEOS) as a modified release (MR) agent. The effect of the prepared sulfonylurea compounds against the diabetic condition was investigated using specific selected biomarkers as of liver enzyme activities as transaminases (AST, ALT) and alkaline phosphatase (ALP), lipids profiles; total cholesterol (TC), triacylglycerols (TG) and total lipid (TL). The antioxidants, oxidative stress biomarkers and histological examination were also examined and discussed., (Copyright © 2019 Elsevier Inc. All rights reserved.)

The aim of this work was the estimation of resveratrol content in two successive extracts (EtOAc and MeOH) of peanuts (Arachis hypogaea L.) pericarp of Egypt, by TLC and HPLC methods. Results showed the presence of 3.0 and 0.5 microg/mL resveratrol in EtOAc and MeOH extracts respectively. The in vitro carbohydrate hydrolyzing enzyme inhibition activity showed higher percentage of inhibition of alpha-amylase, alpha-glucosidase and beta-galactosidase with EtOAc (4.32, 5.93 and 13.7%) than with MeOH extract (3.9, 4.9 and 14.1%) but lower than the standard resveratrol concentration (5.18, 5.94 and 13.26%) and the reference acarbose (5.88, 5.9 and 13.0%). It could be concluded that the content of resveratrol in peanut pericarp is related to the percentage of inhibition activity of carbohydrate hydrolyzing enzymes. These results strongly reflect the benefit of using peanut pericarp, the waste product, as a natural antidiabetic agent.

The present study aims to clarify the protective effect of supplementation with some antioxidants, such as idebenone (200 mg/kg, ip), melatonin (10 mg/kg, ip) and arginine (200 mg/kg, ip) and their combination, on liver function (T. protein, albumin, alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase), energetic parameters (adenosine triphosphate, adenosine diphosphate, adenosine monophosphate, inorganic phosphate, total adenylate, adenylate energy charge and potential phosphate). The effect on glycolytic and glycogenolytic enzymes (glucose, glycogen, glycogen phosphorylase, pyruvate kinase and phosphofructokinase against hypoxia) was also studied. The drugs were administered 24 and 1 h prior sodium nitrite intoxication. All biochemical parameters were estimated 1 h after sodium nitrite injection. Injection of sodium nitrite (75 mg/kg, sc) produced a significant disturbance in all biochemical parameters of liver function, energetic parameters and glycolytic and glycogenolytic enzymes. Hepatic damage was confirmed by histopathological examination of the liver as compared to controls. The marked changes in hepatic cells induced by sodium nitrite were completely abolished by pretreatment with the drug combination, suggesting potential protection against sodium nitrite-induced hypoxia. It could be concluded that a combination of both idebenone and melatonin or idebenone and arginine provides potential protection against sodium nitrite-induced hypoxia by improving biochemical parameters and preserving liver histology.

Objective: It is well documented that oxidative stress is a basic mechanism behind the development of diabetic state. The current study was undertaken to elucidate the hypoglycemic role of zinc, selenium and vitamin E and their mixture in comparison with the antidiabetic drug glibenclamide., Materials and Methods: Male Wistar rats weighing 250 +/- 50 g were made diabetic by injection with a single i.p. dose of streptozotocin (STZ) (65 mg/kg b. wt). Diabetic groups were simultaneously i.p. injected either with zinc chloride (ZnCI2) (5 mg/kg) or with selenium and vitamin E (1.5 mg/kg as sodium selenite and vitamin E 1000 mg/kg) or with zinc, selenium and vitamin E each element i.p. injected according to its corresponding therapeutic dose daily for one month. Another group was orally treated daily with glibenclamide drug (5 mg/kg) for one month., Results: Blood and tissue samples were collected at day 3 post STZ injection (from one group serum glucose level significantly elevated < or = 300, p < or = 0.05) and at day 30 post-treatment in other groups. Liver function, nitric oxide (NO), malondialdehyde (MDA) and phosphoenol pyruvate carboxykinase (PEPCK) were significantly increased, while superoxide dismutase (SOD), reduced glutathione (GSH), total protein, lactate dehydrogenase (LDH), pyruvate kinase (PK) and hexokinase (HK) were inhibited after STZ treatment. Histological examination of diabetic liver showed necrosis and degenerative changes of hepatocytes. Treatment of diabetic rats with ZnCI2, selenium and vitamin E or their combination blunted the increment in serum glucose induced by STZ, preserved liver architecture and ameliorated all the previous mentioned biochemical parameters., Conclusions: It was found that, the combined administration of zinc, selenium and vitamin E exhibited a more remarkable effect than either zinc or selenium and vitamin E. So, the results clearly indicate the beneficial effects of micronutrients combination in controlling hyperglycemia.