Iranian Journal of Pharmaceutical Sciences

The aim of this study was to investigate the prevalence of Mg deficiency and effectof aminophylline infusion on urine magnesium concentration after magnesiumloading test (MLT). To determine serum Mg, venous blood specimens were obtainedjust before the first MLT. Two MLTs were performed. The first one was donebefore starting aminophylline infusion and the 2ndone was done during aminophyllineinfusion. Urine samples were collected from the starting of Mg infusion in each phase.Although low serum Mg was present only in 2 patients, MLTshowed Mg deficiencyin 18 patients. MLTdetected Mg deficiency in 13 out of 14 patients with normalserum Mg, in 2 out of 2 subjects with serum hypomagnesemia, and in 3 out of 5 caseswith serum hypomagnesemia. There was no relationship between Mg retention, ageand serum Mg concentrations. Aminophylline administration increased the 24-h urineMg concentration by 29.3%.

Purpose of this study was to investigate the effect of the presence of the watersoluble polymers viz HPMC, PVPand PEG 6000 on aqueous solubility andcomplexation abilities of felodipine with or without presence of β-cyclodextrin (βCD)and HPβCD by phase solubility studies. The data revealed the initial increase in drugsolubility followed by plateau in the presence of relatively low polymer concentrationi.e. 0.25-0.5 %w/v. Phase solubility diagrams of felodipine in ternary systemshowed similar behaviour to binary system without βCD. Addition of water solublepolymer to βCD solution improved βCD solubilizing efficiency due to increase inβCD complexing power toward felodipine. In binary system solubility was found2.5 to about 10 times higher than in water which was further improved in thepresence of 0.25% w/v water soluble polymer. Ternary systems with βCD showedhighest increments in solubility towards felodipine, with 78.8%, 81.8% and 74%improvement after the addition of 0.25% w/v HPMC, PVPand PEG6000,respectively. Our study confirmed that addition of small amounts of hydrophilicpolymer is useful strategy for improving the solublization and complexing abilitiesof cyclodextrins thus allowing less cyclodextrin to be needed to solubilize givenamount of drug. This offers economic advantage. All the polymers under studyshowed synergistic effect on felodipine cyclodextrin solublization by increasingcomplexation efficiency.The highest solubility improvement up to 81.8% wasobtained for βCD ternary system when 0.25% w/v of PVPwas used.

The complex formed as a consequence of the interaction between the electron-acceptor P-chloranilic acid and an electron donor tamoxifen citrate was employedin the assay of the drug in pure powder and tablets. Chloranilic acid was found toform a charge-transfer complex in a 1:1 stoichiometric ratio, with tamoxifen citrate.The wavelength of maximum absorption for the complex was found to be 550 nmwhile the absorbance was linear over the concentration range of 2-100 g/ml.Evaluations of the various thermodynamic parameters by means of the Scottequation was carried out and were found to decrease with increase in temperature.The free energy change (ΔG°) and the enthalpy of formation (ΔH°) as well as theentropy (ΔS°) were determined for various interactions. Results obtained suggestthat the proposed method may be conveniently applied in the analysis ofcommercially available tamoxifen citrate tablets with a high degree of accuracy andreproducibility.

The cellular therapy and nerve tissue engineering will probably become a majortherapeutic strategy for promoting axonal growth through injured area in centralnervous system and peripheral nervous system in the coming years. The stem cellcarrier scaffolds in nerve tissue engineering resulted in strong survival of cells andsuitable differentiation into neural cells, so this pathway should be created afavorable environment for axon regeneration. Poly lactic-co-glycolic acid (PLGA)has been widely used for manufacturing three dimentional scaffolds for tissueengineering. The pluripotent nature and proliferative capacity of embryoniccarcinoma cells such as P19 also makes them an attractive cell source for tissueengineering. This study was initiated to evaluate potential of biodegradable PLGAmicrospheres for P19-derived neurons for neural tissue engineering and axonregeneration. The PLGAmicrospheres were prepared by using solvent evaporation,water in oil in water, technique. The water phase was polyvinyl alcohol (PVA) solutionand the oil phase was PLGAsolution. Retinoic acid (RA) was added to bacterial dishesas a differentiation factor inducer. P19 cells were attached to the PLGAmicrospheresand differentiated into neural cells on them. PLGAmicrospheres were characterisedfor size and surface morphology by scanning electron microscopy. Thein vitroexperimental studies were performed via immunoflouresent staining, scanningelectron microscopy (SEM), RT-PCR, and histology. The photomicrograph andhistology staining show the surrounded microspheres by P19 cells. The SEMresults demonstrated the attachment and axon formation. Immunoflouresent stainingand RT-PCR analysis for MapII, β-Tubulin, Nestin and Pax6 indicated the differ-entiation of P19 cells into neural cells. This report shows that high surface area alsoallows rapid cell expansion and increases cell attachment on PLGAmicrospheres,so each microsphere contains high cell density that resulted in survival of transplan-tation into the straitum of host animals, therefore, PLGAmicrospheres can help thedifferentiation of P19 cells into neural cells.

This study was designed to explore the protective effects of ascorbic acid andwater extract of Spirulina platensis(blue green algae) on methotrexate-induced lipidperoxidation using goat liver as the lipid source. This in vitroevaluation was doneby measuring the malondialdehyde, 4-hydroxy-2-nonenal, reduced glutathione andnitric oxide content of tissue homogenates. The study reveals the lipid peroxidationinduction capacity of methotrexate, the anti-peroxidative potential of ascorbic acidand aqueous extract of S. platensison methotrexate-induced lipid peroxidation.

The anti-apoptotic gene bcl-2 is located in mitochondria, but it is uncertainwhether its expression affects hepatocyte survival in ischemia/reperfusion (I/R) injury.This experiment was designed to evaluate the role of folic acid in expression of bcl-2in I/R in rat liver. Eighteen Wister rats were divided into sham-operated controlgroup (C) (n=6), I/R group (n=6), folic acid treated group which received 1mg/kg/day folic acid by oral route for 7 days before induction of I/R (n=6). Bcl-2expression was measured by RT-PCR and western blot methods. Folic acidsignificantly increased Bcl-2 mRNAexpression in comparison to the I/R group.Quantification of apoptotic and necrotic hepatocytes, measured by fluorescencemicroscopy and terminal deoxynucleotidyl transferase (TdT)-mediated dUDP-biotin nick end labeling (TUNEL) method, showed a significant decrease inapoptosis and necrosis of hepatocytes in folic acid-treated group. Histopathologi-cal examination of the liver revealed that folic acid protected from severe hepaticdegeneration from I/R injury. The biochemical parameters like alanine transaminasesand aspartate transaminases were significantly decreased in folic acid-treated groupcompared to I/R group. In conclusion, folic acid afforded significant protection againstI/R injury due to its ability to inhibit I/R-induced apoptosis.

In view of potential biological activities of small molecule polyamides, wesynthesized some novel N-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamide (7a,b), and N-(2-(1-benzyl-2-(alkylthio) -1H-imidazole- 5-carboxamido)ethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamides (8a,b) as antitumoragents. The antitumor activity of compounds 7a,band 8a,bwas studied atconcentrations of 0.01, 0.1 and 1 mg/ml, using the potato disk bioassay technique.Vincristine at 0.25 mg/ml employed as positive control and had -67.24% tumorinhibition. Maximum % inhibition for potato tumors was found to be -75.52 for 7bat 1 mg/ml.

Keeping in view the promising potential of carbonic anhydrase inhibitor based antimicrobials and enhancement of carbonic anhydrase inhibitory activity by metal complexes of sulfonamides, with an aim to develop better antimicrobial agents we have attempted investigation of antimicrobial activity of metal complexes of 4-(2'-hydroxy phenyl imino) phenyl sulphonamide. Sulfanilamide was taken as the starting material to synthesize 4-(2'-hydroxy phenyl imino) phenyl sulphonamide.Cu (II), Zn (II), Co (II), Ni (II) and Pb (II) complexes were synthesized following reported methods. The in vitroscreening was carried out using two gram positive bacteria (S. aureus, E. faecalis) and two gram-negative bacteria (E. coli, P.aeruginosa) by disc diffusion method. Metal complexes were found to enhance the antimicrobial potental of the ligand.

A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, mass pectra and elemental analysis. Compounds 2-9 were screened for anti-nociceptive, anti-inflammatory and antiepileptic activity by AcOH induced writhing method ,carrageenan induced paw edema method and maximal electroshock induced convulsion method respectively. Out of the eight synthesized compounds, indeno[1,2-b]quinoxalin-11-ylidine (4-nitrophenyl)amine (3) exhibited promising anti-inflammatory activity and anti-nociceptive activity. N-(2,4-dinitrophenyl)-N'-(indeno[1,2-b]quinoxalin-11-ylidene)hydrazine (7) showed promising anti-inflammatory activity, anti-nociceptive activity, and antiepileptic activity, whereas N4-indeno[1, 2-b]quinoxalin-11-ylidene biphenyl-4,4'-diamine (8) showed promising anti-inflammatory activity.