Non-steroidal anti-inflammatory drugs (NSAIDs) induce tissue damage and oxidative stress in animal models of stomach damage. In the present study, the protective effects of wheat peptides were evaluated in a NSAID-induced stomach damage model in rats. Different doses of wheat peptides or distilled water were administered daily by gavage for 30 days before the rat stomach damage model was established by administration of NSAIDs (aspirin and indomethacin) into the digestive tract twice. The treatment of wheat peptides decreased the NSAID-induced gastric epithelial cell degeneration and oxidative stress and NO levels in the rats. Wheat peptides significantly increased the superoxide dismutase (SOD) and glutathione peroxidase (GPx) activities and decreased iNOS activity in stomach. The mRNA expression level of μ-opioid receptor was significantly decreased in wheat peptides-treated rats than that in in the control rats. The results suggest that NSAID drugs induced stomach damage in rats, wchih can be prevented by wheat peptides. The mechanisms for the protective effects were most likely through reducing NSAID-induced oxidative stress.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; adverse effects ; Antioxidants ; pharmacology ; Aspirin ; adverse effects ; Gastric Mucosa ; drug effects ; Gene Expression ; Glutathione Peroxidase ; drug effects ; Indomethacin ; adverse effects ; Male ; Nitric Oxide ; biosynthesis ; Nitric Oxide Synthase ; chemical synthesis ; Oxidation-Reduction ; Oxidative Stress ; drug effects ; Plant Proteins ; pharmacology ; RNA, Messenger ; genetics ; Rats ; Rats, Sprague-Dawley ; Receptors, Opioid, mu ; drug effects ; Stomach ; drug effects ; Superoxide Dismutase ; drug effects ; Triticum ; chemistry

A series of adefovir mono-L-amino acid esters, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs with more potent anti-HBV activity and lower nephrotoxicity were designed and synthesized. Adefovir bis (L-amino acid) ester was used as lead compound, according to pathological and pharmacological findings that non-steroidal anti-inflammatory drugs can effectively inhibit the organic anion transporter 1 (hOAT1)-mediated adefovir phosphonic acid pairs of anion transport across tubular basement membrane thereby reducing the nephrotoxicity of adefovir. Flatten design principle was used to introducing non-steroidal anti-inflammatory drugs structural fragments to design and synthesize target adefovir mixture ester prodrugs. HepG2 2.2.15 cell line was used as in vitro anti-HBV activity evaluation model. Five compounds exhibited antiviral activity, and compound 18 showed the most potent anti-HBV activity and relatively high selective index (EC50 3.92 micromol L(-1), SI 9.97). HK-2 cell line was used as in vitro model to evaluate nephrotoxicity. Results suggested the target compounds have lower cytotoxicity than the positive control. Moreover, by analyzing the primary structure and activity relationship of these compounds, it could suggest that mono-L-amino acid ester, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.
Adenine ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Amino Acids ; chemical synthesis ; chemistry ; pharmacology ; Anti-Inflammatory Agents, Non-Steroidal ; chemical synthesis ; chemistry ; pharmacology ; Antiviral Agents ; chemical synthesis ; chemistry ; pharmacology ; Carboxylic Acids ; chemistry ; pharmacology ; Cell Survival ; drug effects ; Drug Design ; Hep G2 Cells ; drug effects ; Humans ; Kidney Tubules, Proximal ; cytology ; metabolism ; L-Lactate Dehydrogenase ; metabolism ; Molecular Structure ; Organophosphonates ; chemical synthesis ; chemistry ; pharmacology ; Prodrugs ; chemical synthesis ; chemistry ; pharmacology

Tepoxalin is a potent inhibitor of both the cyclooxygenase and lipoxygenase pathways of the arachidonic acid cascade, as well as a potent anti-inflammatory and control-pain (postoperation, arthritis et. al.) agent. The new method about the use of novel synthesis reagents and the first using ionic liquid as reactive solvent to synthesize tepoxalin were presented in this paper. The ionic liquid can be easily recycled and reused for several runs efficiently. The analgesic activity of tepoxalin was detected by acetic acid test on mice. The analysis of variance showed that oral administration of tepoxalin could significantly inhibit the number of writhing response within 1 hour and prolong the latent time in a dose dependent manner as compared with CMC control group (P < 0.05). At the same time, tepoxalin had the same analgesic activity as diclofenac sodium.
Administration, Oral ; Analgesics ; administration & dosage ; chemical synthesis ; pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; chemical synthesis ; pharmacology ; Cyclooxygenase Inhibitors ; administration & dosage ; chemical synthesis ; pharmacology ; Diclofenac ; pharmacology ; Imidazoles ; chemistry ; Ionic Liquids ; chemistry ; Lipoxygenase Inhibitors ; administration & dosage ; chemical synthesis ; pharmacology ; Mice ; Pain Measurement ; drug effects ; Pyrazoles ; administration & dosage ; chemical synthesis ; pharmacology ; Random Allocation

A new pyranocoumarin as an analogue of calophyllolide, compound 6, is firstly prepared and reported to have potent anti-inflammatory activity on carrageenin-induced edema in rats.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; chemical synthesis ; chemistry ; therapeutic use ; Carrageenan ; Coumarins ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use ; Edema ; chemically induced ; drug therapy ; Male ; Molecular Structure ; Rats ; Rats, Wistar

Fluidized-bed manufactured enteric-coated diclofenac sodium pellets were compressed into tablets. The blend of two aqueous acrylic resins dispersion in different ratios, Eudragit NE30D and Eudragit L30D-55, were used to prepare enteric-coated diclofenac sodium pellets of different particle sizes and coating level. The cushioning pellets with different properties and these enteric-coated pellets were compressed into tablets in different proportions. The drug release of the tablets containing these pellets would be lower than 10% in 2 h in simulated gastric fluid, but reach (83 +/- 2.42)% in 1 h in simulated enteric fluid. The mixture of Eudragit NE30D and Eudragit L30D-55 could be used to prepare enteric pellets which are suitable for compression. The cushioning pellets which were composed of stearic acid/microcrystalline cellulose (4:1, w/w) could avoid rupture of the coating of pellets during the compression.
Acrylic Resins ; chemistry ; Anti-Inflammatory Agents, Non-Steroidal ; chemical synthesis ; Cellulose ; chemistry ; Diclofenac ; chemical synthesis ; Drug Carriers ; Drug Compounding ; methods ; Drug Delivery Systems ; Methacrylates ; chemistry ; Particle Size ; Polymers ; chemistry ; Solubility ; Tablets, Enteric-Coated ; chemistry

Sugar-containing monomer vinylbenzylglycosylallyamide (VBG) was synthesized by vinylbenzyl amine and delta-gluconolactone in dimethylformamide(DMF) solution. The sugar-based hydrogel was prepared by free radical crosslinking copolymerization of VBG, itaconic acid (IA) and acrylamide (AM). The release properties of Aspirin from xerogels matrices and from hydrogel in different pH solutions and different concentration NaCl solutions were studied respectively. The release mechanism of Aspirin was further confirmed by evaluating the n value in Peppas equation. The results indicated that the drug release increased with the increase of pH values and with the decrease of NaCl concentration.
Acrylic Resins ; chemistry ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; chemistry ; Aspirin ; administration & dosage ; chemistry ; Delayed-Action Preparations ; chemical synthesis ; chemistry ; Humans ; Hydrogel, Polyethylene Glycol Dimethacrylate ; chemical synthesis ; chemistry ; Hydrogen-Ion Concentration ; Succinates ; chemistry ; Vinyl Compounds ; chemistry

Hydroxyethyl chitin (HECH) is a water soluble chitin derivative made by etherification of chitin, ethylene chlorohydrin was used as etherification reagent in this reaction. A novel interpenetrating polymer network (IPN) composed of HECH/PAA was prepared. The IR spectra confirmed that HECH/PAA was formed through chemical bond interaction. The sensitivity of this hydrogel to temperature and pH was studied. The swelling ratio of this hydrogel in artificial intestinal juice is much greater than that in artificial gastric juice. The IPN hydrogel exhibited a typical pH-sensitivity, and its degree of swelling ratio increased with the increase of temperature. The sustained-release drug system of Dichlofenac potassium was prepared by using HECH/PAA as the drug carrier. The release experiment showed a perfect release behavior in artificial intestinal juice. This IPN is expected to be used as a good drug delivery system of enteric medicine.
Acrylates ; administration & dosage ; chemistry ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; Chitin ; administration & dosage ; analogs & derivatives ; chemistry ; Delayed-Action Preparations ; Diclofenac ; administration & dosage ; Drug Carriers ; chemical synthesis ; Drug Delivery Systems ; Hydrogel, Polyethylene Glycol Dimethacrylate ; administration & dosage ; chemistry ; Hydrogen-Ion Concentration

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; chemical synthesis ; chemistry ; pharmacology ; Antidepressive Agents ; chemical synthesis ; chemistry ; pharmacology ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Pyrroles ; chemical synthesis ; chemistry ; pharmacology

To further understand triptolide, this paper has introduced the pharmacology, pharmacokinetics, toxicity, the clinic application and semi-synthesis of triptolide on basis of importance and significant contents of reference which have been consulted in the past twenty years. Presently triptolide and Tripterygium wilfordii have been a hot spot of modernization of Chinese traditional medicine. It is very important to develop a new dosage form of high effect and low toxicity by making use of advanced technology according to its characteristics.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Antineoplastic Agents, Alkylating ; pharmacology ; Antispermatogenic Agents ; pharmacology ; Diterpenes ; chemical synthesis ; isolation & purification ; pharmacology ; toxicity ; Epoxy Compounds ; Humans ; Immunosuppressive Agents ; pharmacology ; Phenanthrenes ; isolation & purification ; pharmacology ; toxicity ; Tripterygium ; chemistry

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Cell Line, Tumor ; drug effects ; Diterpenes ; chemical synthesis ; isolation & purification ; pharmacology ; Epoxy Compounds ; Humans ; Phenanthrenes ; chemical synthesis ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Tripterygium ; chemistry