Design, synthesis and evaluation of D-galactose-beta-cyclodextrin conjugates as drug-carrying molecules.

Several kinds of D-galactose-beta-cyclodextrin conjugates having a phenyl group in the spacers between the D-galactose and beta-cyclodextrin were designed and synthesized as drug-carrying molecules. Their evaluation as drug-carrying molecules was done by measuring the molecular interactions with the anticancer agent, doxorubicin, and with the d-galactose-binding peanut lectin using an SPR optical biosensor. The SPR analyses showed that these conjugates had remarkably high inclusion associations of 10(5) approximately 10(7)M(-1) levels for the immobilized doxorubicin. Their association constants for immobilized peanut lectin were at the level of 10(4) approximately 10(5)M(-1), as we expected. These conjugates will be useful drug-carrying models which can site-specifically carry doxorubicin to the cells containing D-galactose-binding lectin.

Analysis by partial reflection spectrometry of protonated tetraphenylporphyrin adsorbed at a liquid-liquid interface.

Visible reflection spectra of diprotonated meso-tetraphenylporphyrin adsorbates spontaneously formed at a dodecane-aqueous sulfuric acid interface have been measured using a home-made device comprising a prism-cell and variable-angle optics. The tilt angle of the pyrrole ring plane was estimated to be 47 degrees from the interface normal by use of an experimentally evaluated molecular density (1.20x10(-10) mol cm(-2)) of the diprotonated molecule in a monolayer form at the liquid-liquid interface. Positive and negative bands have been observed in the p-polarized partial internal reflection (p-PIR) spectra, whose band locations correspond to those in p-polarized external reflection (p-ER) spectra. Nevertheless, the bands in the p-PIR exhibited reversed sign to those of p-ER spectra. These suggest that the surface selection rule of the p-PIR spectrometry has a reversal rule of p-ER and p-PIR can also be used for the analysis of molecular orientation.