Ultrasonic study of hyaluronan interactions with Septonex-A pharmaceutical cationic surfactant.

Interactions between hyaluronan and the cationic surfactant Septonex were studied using high resolution ultrasound spectroscopy. Four different interaction regions were identified in aqueous solution in a narrow interval of surfactant concentrations. In contrast, in 0.15 mol/L NaCl solution, essentially only two principal regions were observed. Hyaluronan-Septonex aggregates were generally less compressible than Septonex monomers or micelles and their formation in water was not appreciably affected by hyaluronan molecular weight. In the presence of NaCl, the effect of hyaluronan molecular weight was more profound, which can be ascribed to its conformational sensitivity to ionic strength combined with its role as a surfactant counterion. Hyaluronan-Septonex interactions were closer to interactions with CTAB than with TTAB. Differences in structure or Krafft temperature (solubility) between Septonex and CTAB were thus not significantly reflected in these interactions. The basic characteristics of Septonex surfactant were also determined.

Densitometry and ultrasound velocimetry of hyaluronan solutions in water and in sodium chloride solution.

The densities of hyaluronan solutions in water and 0.15M NaCl were measured in the temperature range from 25 to 50°C for the hyaluronan molecular weights from 10 to 1,750 kDa. The density increased linearly with concentration and decreased with temperature. The data were fitted by the equation describing the density as a linear function of concentration and a quadratic function of temperature. The effect of molecular weight was negligible and thus single equation was sufficient to describe all data. The apparent and partial specific volumes were calculated from the density data including their extrapolated values to infinite dilutions. The measurement of ultrasound speed in the same solutions under the same conditions enabled to calculate the compressibility and its dependence on concentration and temperature. The compressibility decreased with both the concentration and the temperature but the effect of the concentration was only slight mild. The compressibility was used to estimate the hydration numbers which slightly decreased with increasing temperature and concentration. The addition of NaCl changed only the numerical values of density and ultrasound velocity while not changing the character of their dependence on temperature and concentration. Measured and calculated data indicate that hyaluronan does not disturb the specific water structure in the studied concentration range and support the idea of the existence of water clusters or nanodroplets hydrating the hyaluronan chains in solution.

Substances with antineoplastic activity. XCVI. Some pharmacological properties and therapeutic synergism of 6-purinyl-N-(2-chloroethyl)thiocarbamate with cytosine arabinoside.

The cancerostatic effect of 6-purinyl-N-(2-chloroethyl)thiocarbamate (Cloturin VUFB, VUFB-15686) was studied in detail in mice and rats bearing transplantable tumors. The cytotoxic activities were measured by determining the incorporation rate of 5-iodo-2'-deoxy[6-3H]uridine and uniformly labeled [U-14C]amino acid mixture into trichloroacetic acid-insoluble fraction of Yoshida ascites reticulosarcoma cells during a short-term incubation with the drug. From the results obtained it follows that the new substance is therapeutically more effective in comparison with 6-mercaptopurine (NSC-755). A therapeutic synergism of Cloturin with cytosine arabinoside (NSC-63978) was observed.