Nebulization of mycophenolate mofetil inhalation suspension in rats: comparison with oral and pulmonary administration of Cellcept®.

In this study, a suspension of mycophenolate mofetil (MMF) suitable for inhalation was developed using the emulsion template process and characterized for particle size and aerosolization performance. To evaluate the benefits of this suspension over a solution, the IV Cellcept(®) solution was also characterized in vitro. Both formulations exhibited excellent aerosolization performance.

Biotinylation of an enkephalin-containing heptapeptide via various spacer arms. Synthesis, comparative binding studies toward avidin, and application as substrates in enzymatic reactions.

The preparation of an enkephalin-containing heptapeptide of the sequence Tyr-Gly-Gly-Phe-Leu-Arg-Arg-OH with a biotinyl moiety linked to the carboxy terminus is described. A series of biotinylated derivatives, each containing a different linker (LC) moiety between the biotin function and the carboxyterminal Arg residue, were synthesized by solution-phase chemistry following the coupling of the side chain protected peptide with previously prepared appropriate biotinylamine derivative. Both linear and flexible spacer arms of variable chain lengths [LC = (CH2)x, x = 2, 4, or 6] as well as semirigid cyclohexyl spacers (racemic 1,2-cyclohexane, cis or trans) were incorporated.

Synthesis, biological activity, conformational analysis by NMR and molecular modeling of N-formyl-L-Met-L-Pro-L-Phe-OMe, a proline analogue of the chemotactic peptide N-formyl-L-Met-L-Leu-L-Phe-OH.

The tripeptide N-formyl-Met-Pro-Phe-OMe (f-MPF-OMe), an analogue of the signal peptide N-formyl-Met-Leu-Phe-OH (f-MLF-OH), was synthesized and its chemotactic activity evaluated; it showed no activity in either superoxide production or calcium mobility with human neutrophils. However, the corresponding acid f-MPF-OH retained about 25% activity in the production of superoxide. The conformation of the f-MPF-OMe analogue was evaluated by NMR spectroscopy and molecular simulation and shown to predominate in a gamma-turn with a hydrogen bond between Met CO and Phe NH.

Structure of a psoralen derivative of a monosubstituted 18-crown-6 ether.

N-[(2,5,9-Trimethyl-7-oxo-7H-furo[3,2-g]-[1] benzopyran-3-yl)methyl]-1,4,7,10,13,16-hexaoxacyclooctadecane- 2,3-dicarboximide, C29H35NO11, Mr = 573.60, monoclinic, P21, alpha = 18.877 (9), b = 6.

Catalase activity measurement with the disk flotation method.

Activity measurements of catalase are usually performed with a spectrophotometric method by monitoring the decrease of H2O2 at 240 nm. A different method presented here uses an instrument named Catalase-meter and yields flotation time data which are expressed in tenth of seconds. For the first time, solutions of catalase of different concentrations were tested simultaneously with the two methods, and the Catalase-meter's flotation data were submitted to correlation with international units calculated from spectrophotometric data.