benzofurans and Carbon-Tetrachloride-Poisoning

The aims of this study were to demonstrate the hepatoprotective activity of herpetin (HPT) and the enhanced hepatoprotective efficiency of liposomal herpetin against carbon tetrachloride-induced liver injury in mice.. Herpetin was isolated from Herpetospermum seed and identified by ESI-MS and NMR. To enhance liver targeting and improve solubility of HPT, liposomal HPT was prepared with optimal formulation. The intravenous injection safety of the liposomes was then evaluated. Further, the hepatoprotective effects of liposomal HPT on model mice were investigated by the comparison of different liver marker enzymes and histopathological examination.. The prepared HPT liposome showed spherical or ellipsoidal vesicles with the entrapment efficiency of 94.50 ± 2.15% and particle size of 119.2 ± 10.7 nm. After 4 days intravenous administration of liposomal herpetin, no obvious damage could be observed at the injection site of each group. The liposomal HPT has no destructive effect on erythrocytes and little influence on whole blood clotting time. Free HPT exhibited only a weak protective function to model mice, whereas an enhanced hepatoprotective activity was observed using liposomal herpetin for treatment.. The hepatoprotective efficiency of herpetin is able to be promoted through pharmaceutical application of liposome and liposomal herpetin is a promising new medicine for hepatoprotection.

Topics: Animals; Benzofurans; Blood Circulation Time; Carbon Tetrachloride Poisoning; Chemical and Drug Induced Liver Injury; Cucurbitaceae; Erythrocytes; Injections, Intravenous; Liposomes; Liver Function Tests; Magnetic Resonance Spectroscopy; Male; Mice; Mice, Inbred ICR; Particle Size; Protective Agents; Seeds; Spectrometry, Mass, Electrospray Ionization

In the course of searching hepatoprotective agents from natural sources, the protective effect of chemical constituents of the marine brown alga Spatoglossum variabile Figaro et DE Notar (Dictyoaceae) against CCl₄-induced liver damage in Wistar rats was investigated. The compounds were first investigated for in vitro radical scavenging potential and were also tested for β-glucuronidase inhibition to further explore the relationship between hepatoprotection and antiradical potential.. The compounds cinnamic acid esters 1 and 2 and aurone derivatives 3 and 4 were first investigated for in vitro radical scavenging potential against 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH), and superoxide anion radicals. In vivo hepatoprotective studies were performed in seven groups (n = 6) of Wistar rats. The test groups were pretreated with compounds (10 mg/kg body weight, po) orally for 30 min before the intraperitoneal administration of a dose of 20% CCl₄ diluted with dietary cooking oil. Moreover, compounds were also tested for β-glucuronidase inhibition to explore the relationship between hepatoprotection and radical scavenging potential.. The test compounds 1-4 were found to exhibit antiradical activity against 1,1-diphenyl-2-picrylhydrazyl radicals with IC₅₀ values ranging between 54 and 138 µM, whereas aurone derivatives 3 and 4 additionally exhibited superoxide anion scavenging effects with IC₅₀ values of 95 and 87 µM, respectively. In addition, these compounds were found to be weak inhibitors of xanthine oxidase (IC₅₀ ≥1000 µM). In animal model, pretreatment with compounds 2-4 significantly blocked the CCl₄-induced increase in the levels of the serum biochemical markers.. It appears that the hepatoprotection afforded by these compounds was mainly due to their radical scavenging activity that protected the cells from the free radicals generated by CCl₄-induced hepatotoxicity.

Topics: Animals; Benzofurans; Biomarkers; Carbon Tetrachloride Poisoning; Cell Survival; Cinnamates; Drug Discovery; Enzyme Inhibitors; Escherichia coli Proteins; Free Radical Scavengers; Glucuronidase; Humans; Liver; Male; Milk Proteins; Neutrophils; Phaeophyceae; Rats; Rats, Wistar; Xanthine Oxidase

The methanol extract of the Oriental medicinal plant Vitis coignetiae (Vitaceae) showed hepatoprotective activity in the in vitro assay method using primary cultured rat hepatocytes. Activity-guided fractionation of the extract afforded epsilon-viniferin as an active principle. The protective effect of epsilon-viniferin against mice carbon tetrachloride-induced hepatic injury in mice was shown by serum enzyme assay as well as by pathological examination. In addition to epsilon-viniferin, plant oligostilbenes, ampelopsins A, C, F and the mixture of vitisin A and cis-vitisin A were also present in the extract. Among them, ampelopsin C and the mixture of vitisin A and cis-vitisin A were found to be powerful hepatotoxins.

Topics: Animals; Benzofurans; Carbon Tetrachloride Poisoning; Chemical and Drug Induced Liver Injury; Liver Diseases; Male; Mice; Molecular Structure; Plants, Medicinal; Stilbenes

IRFI 016 has demonstrated significant antioxidant activity, inhibiting hepatic lipid peroxidation (rat intoxicated by CCl4) and the formation of gastric lesions by ethanol (rat). This activity proved equal to or better than that exhibited by the most investigated antioxidant/radical scavenger agents (such as BHA, BHT, Vitamin E). The drug markedly increased mucus production (rabbit, mouse) by all the administration routes used (os, i.v. and inhalatory) and proved more active than, or overlapping, the most noted mucoregulatory/mucolytic drugs (sobrerol, bromexine, thiopronine, ambroxol, N-acetylcysteine) which were chosen for comparison. The tracheo-bronchial mucus viscosity was also significantly reduced (bronchitic animals) as was the fucose and total protein content. In the pigeon, IRFI 016 improved mucociliary clearance. Moreover IRFI 016 evidenced anti-inflammatory activity nearly equal to that exhibited by ASA and phenylbutazone (carrageenin oedema, abcesses and inflammatory pain).

Topics: Abscess; Animals; Antioxidants; Benzofurans; Bronchi; Carbon Tetrachloride Poisoning; Carrageenan; Columbidae; Edema; Ethanol; Expectorants; Female; Lipid Peroxidation; Liver; Male; Mice; Mice, Inbred Strains; Mucus; Pain; Rabbits; Rats; Rats, Inbred Strains; Stomach; Trachea; Vitamin E