Betulin-3,28-diphosphate. Physico-Chemical Properties and In Vitro Biological Activity Experiments

Melnikova, N.B.; Malygina, D.S.; Klabukova, I.N.; Belov, D.V.; Vasin, V.A.; Petrov, P.S.; Knyazev, A.V.; Markin, A.V.

Авторы: Melnikova Nina B., Malygina Darina S., Klabukova Irina N., Belov Denis V., Vasin Viktor A., Petrov Pavel S., Knyazev Alexander V., Markin Alexey V.
Журнал: Molecules
Том: 23
Номер: 5
Год издания: 2018
Издательство: MDPI
Местоположение издательства: Basel, Switzerland
Первая страница: 1175
Последняя страница: 1188
DOI: 10.3390/molecules23051175
Аннотация: Abstract Betulin-3,28-diphosphate (BDP) obtained by phosphorylation of betulin using POCl3 has two main structural forms—BDP-1 and BDP-2—which differ in ethanol solubility, melting point, FTIR spectra, thermoanalytical characteristics and biological activity. Betulin-3,28-diphosphate and its sodium salt (Na-BDP) were characterized using 13C and 31P-NMR spectra, powder XRD experiments, as well as differential scanning calorimetry (DSC) and thermogravimetric analysis (TG) methods. The exo-effects at 193 ± 8 °C for ethanol soluble BDP-1 samples (−19.7 ± 0.2 kJ∙mol−1) were about three times less than for ethanol insoluble BDP-2 samples f (−70.5 ± 0.7 kJ∙mol−1). The DSC curves of Na-BDP-1 and Na-BDP-2 characterized the endo-effects having a maximum at 95–112 °C. Water-soluble Na-BDP-1 was obtained as needle-like crystals, unlike poorly crystalline Na-BDP-2, whereas BDP-1 and BDP-2 aged with time and were isolated as amorphous substances. In vitro experiments on rats showed that compared to the control, Na-BDP-1 increased catalase and SOD activity and improved energy metabolism more effectively than Na-BDP-2.
Добавил в систему: Белов Денис Владимирович

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Betulin-3,28-diphosphate. Physico-Chemical Properties and In Vitro Biological Activity Experimentsстатья

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